Herbicidal sulfonamides

ABSTRACT

Certain substituted pyrimidine sulfonylureas, such as 3-[[[(4-(dimethoxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]aminosulfonyl]-2-thiophenecarboxylic acid, methyl ester, are selective pre-emergence and/or post-emergence herbicides.

RELATED APPLICATION

This application is a continuation of my application Ser. No. 543,835 filed Oct. 20, 1983, which is a continuation-in-part of my application U.S. Ser. No. 434,038, filed Oct. 20, 1982, now abandoned which is a continuation-in-part of U.S. Ser. No. 328,018 filed Dec. 7, 1981, now abandoned.

BACKGROUND OF THE INVENTION

This invention relates to herbicidal sulfonamides, and, more particularly, to (dimethoxymethyl)pyrimidinyl sulfonylurea compounds which are selective pre-emergence and/or post-emergence herbicides.

DESCRIPTION OF THE PRIOR ART

U.S. Pat. Nos. 4,127,405 and 4,169,719 disclose herbicidal methoxymethylpyrimidine sulfonylurea compounds of the type which contain a --CH₂ OCH₃ heterocyclic substituent.

European No. 7687 discloses herbicidal sulfonylurea compounds such as, among others, ##STR1## where X is CH₃ or OCH₃ ;

Z is CH or N; and

Y is C₁ -C₄ alkyl substituted with OCH₃, OC₂ H₅, CN, C(O)L, or 1-3 atoms of F, Cl, or Br, where L is NH₂, OH, N(OCH₃)CH₃, NH(C₁ -C₄ alkyl), N(C₁ -C₄ alkyl) or C₁ -C₆ alkoxy.

U.S. Application Ser. No. 116,920, discloses herbicidal substituted benzenesulfonylureas which contain as the heterocyclic substituent ##STR2## where X is CH₃ or OCH₃ ;

Z is CH or N; and

Y is (among others) C₁ -C₄ alkyl substituted with OC₂ H₅, CN, CO₂ H, CO₂ H₃ or CO₂ C₂ H₅.

J. Am. Chem. Soc., 69, 3072 (1947) teaches compounds of the formula: ##STR3## where A is H or ##STR4## X is Cl, CH₃, CH₃ O, CH₂ OCH₃, or H; and Y is CH(OCH₃)₂ or CH(OC₂ H₅)₂ ;

and their use as antibacterial agents.

SUMMARY OF THE INVENTION

This invention relates to novel compounds of Formula I, suitable agricultural compositions containing them, and their method of use as general and/or selective pre-emergence and/or post-emergence herbicides or plant growth regulants. ##STR5## wherein X is CH₃, OCH₃, Cl, C₂, H₅ or OC₂ H₅ ;

Z is CH or N;

Y is CH₂ OR, CH₂ S(O)_(m) R₁, CH(QR₁)₂, R₁ CHS(O)_(m) R₁, ##STR6## R is H, C(O)R₃, CO₂ R₄, C(O)NR₅ R₆ or ##STR7## R₁ is C₁ -C₂ alkyl; R₂ is --CH₂ CH₂ --, --CH(CH₃)CH₂ -- or --CH₂ CH₂ CH₂ --;

R₃ is C₁ -C₃ alkyl;

R₄ is C₁ -C₃ alkyl;

R₅ is H or CH₃ ;

R₆ is C₁ -C₃ alkyl;

Q is O or S;

m is 0, 1 or 2;

A is ##STR8## R₇ is H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, F, Cl, I, Br, NO₂, CF₃, CO₂ R₉, SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃, OSO₂ R₁₂, S(O)_(n) R₁₃, LCF₃, LCHF₂, LCF₂ CF₂ H, CH₂ Cl, CHCl₂, CH₂ OCH₃ or CH₂ OCH₂ CH₃ ;

R₈ is H, F, Cl, Br, CF₃, NO₂, C₁ -C₃ alkyl C₁ -C₃ alkoxy, OCF₂ H or SCF₂ H;

R₉ is C₁ -C₄ alkyl, CH₂ CH₂ OCH₃, CH₂ CH₂ Cl or CH₂ CH═CH₂ ;

R₁₀ and R₁₁ are independently C₁ -C₃ aklyl;

R₁₂ is C₁ -C₄ alkyl, CH₂ CH₂ OCH₃, CH₂ CH₂ CH₂ OCH₃ or C₁ -C₄ alkyl substituted with 1-3 atoms or F, Cl, or Br;

R₁₃ is C₁ -C₄ alkyl or CH₂ CH═CH₂ ;

n is 0 or 2;

L is O, S or SO₂ ;

R₁₄ is H, CH₃, OCH₃, F, Cl, Br, NO₂, SO₂ N(CH₃)₂, OSO₂ R₁ or S(O)_(n) R₁ ;

R₁₅ is H, Cl, Br, CH₃, OCH₃ or NO₂ ;

R₁₆ is H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, F, Cl, Br, CF₃, CO₂ R₉, SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃ or S(O)_(n) R₁₃ ;

R₁₇ is H, F, Cl, Br, CH₃ or OCH₃ ;

W is O or S;

W₁ is O or S;

R₁₈ is H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, F, Cl, Br, NO₂, CO₂ R₉, SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃ or S(O)_(n) R₁₃ ;

R₁₉ is Cl, NO₂, CF₃, CO₂ R₉, SO₂ N(OCH₃)CH₃, SO₂ NR₁₀ R₁₁, OSO₂ R₁₂, S(O)_(n) R₁₃, C₁ -C₃ alkyl, or C₁ -C₃ alkoxy optionally substituted with 1-5 atoms of Cl or F;

R₂₀ is Cl, NO₂, CF₃, CO₂ R₉, SO₂ N(OCH₃)CH₃, C₁ -C₃ alkyl, OSO₂ R₁₂ or C₁ -C₃ alkoxy optionally substituted with 1-5 atoms of Cl or F;

R₂₁ is H or CH₃ ;

and their agriculturally suitable salts; provided that

(1) the total number of carbon atoms of R₁₀ and R₁₁ is less than or equal to 4;

(2) when X is Cl, then Z is CH;

(3) when W is O, then R₁₈ is H, Cl, Br, CH₃ or CO₂ R₉ ;

(4) when W is O and R₁₈ is H, Cl, Br, or CH₃, then A is ##STR9## and (5) when W₁ is S, then R₂₁ is H and A is ##STR10##

Preferred for their higher herbicidal activity and/or more favorable ease of synthesis are:

(1) Compounds of Formula I where W₁ is O, X is CH₃, OCH₂ CH₃ or OCH₃ and R₂₁ is H;

(2) Compounds of Preferred 1 where Y is CH(QR₁)₂, CH₂ SR₁, CR₁ (QR₁)₂, ##STR11## (3) Compounds of Preferred 2 where Y is CH(QR₁)₂, CH₂ SR₁ or ##STR12## and Q is 0; (4) Compounds of Preferred (3) wherein A is ##STR13## R₇ is C₁ -C₃ alkyl, C₁ -C₃ alkoxy, Cl, NO₂, CO₂ R₉, SO₂ (C₁ -C₃ alkyl), SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃, OSO₂ R₁₃, CH₂ OCH₃ or LCF₂ H;

R₁₄ is CH₃, OCH₃, Cl, OSO₂ CH₃ or SO₂ (C₁ -C₃ alkyl);

R₁₆ is CH₃, OCH₃, Cl, SO₂ CH₃ or SO₂ N(CH₃)₂ ;

R₁₈ is CH₃, Cl, Br, CO₂ R₉ or SO₂ CH₃ ;

(5) Compounds of Preferred (4) where A is ##STR14## and (6) Compounds of Preferred (5) where

R₇ is CO₂ CH₃, CO₂ CH₂ CH₃, SO₂ CH₃, SO₂ CH₂ CH₃, SO₂ N(CH₃)₂, OSO₂ CH₃, OSO₂ CH₂ CH₃ ; and

R₈ is H, F, Cl, CF₃, CH₃ or OCH₃.

Specifically preferred are:

3-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]aminosulfonyl]-2-thiophenecarboxylic acid, methyl ester;

2-chloro-N-[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)-aminocarbonyl]benzenesulfonamide;

2-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

N-[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]-2-methylsulfonylbenzenesulfonamide;

N-[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]-2-nitrobenzenesulfonamide;

2-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]aminosulfonyl)benzoic acid, 2-propyl ester;

2-[[[4-methyl-6-(tetrahydropyran-2-yloxymethyl)pyrimin-2-yl]aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

2-[[[4-(hydroxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

2[[[4-(acetyloxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

2-[[[(4-dimethoxymethyl-6-methoxypyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

5-chloro-2-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

5-chloro-2-[[(4-dimethoxymethyl-6-methoxypyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester;

2-[[(4-(1,3-dioxan-2-yl)-6-methoxypyrimidin-2-yl)aminocarbonyl)aminosulfonyl]benzoic acid, methyl ester; and

2-[[(4-(1,3-dioxolan-2-yl)-6-methoxypyrimidin-2yl)-aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester.

The compounds of this invention are highly active pre-emergence and/or post-emergence herbicides. Certain compounds of this invention are useful for selective weed control in crops such as cotton, soybeans, wheat or corn.

DETAILED DESCRIPTION OF THE INVENTION Synthesis

The compounds of Formula I may be prepared by the reaction of an appropriately substituted sulfonyl isocyanate of Formula II with an appropriate 2-aminoheterocycle of Formula III according to Equation 1: ##STR15## wherein A, X, R₂₁ and Z(O)_(m) are as previously defined;

Y is CH₂ OR, CH₂ SR₁, CH(QR₁)₂ CH(QR₂ Q), CH(R₁)S(O)_(m) R₁, C(R₁)(QR₁)₂ or C(R₁)(QR₂ Q);

R is ##STR16## and m, R₁ and R₂ are as previously defined.

The reaction of Equation 1 is best carried out in an inert aprotic solvent such as methylene chloride, tetrahydrofuran, acetonitrile at a temperature between 20° and 80°. A catalytic amount of DABCO (1,4-diazabicyclo[2.2.2]octane) may be used to accelerate the reaction. In the cases in which the products are insoluble in the reaction solvent, they may be isolated by simple filtration. When the products are soluble in the reaction solvent they are isolated by evaporation of the solvent and trituration of the residue with solvents such as 1-chlorobutane, ethyl ether or methanol and filtration.

Preparation of isocyanates (II) is described in the following: U.S. Pat. No. 4,127,405, U.S. Pat. No. 4,169,719, Eur. Pat. No. 7,687, Eur. Pat. No. 13,480, Eur. Pat. No. 23,141, Eur. Pat. No. 23,422, Eur. Pat. No. 30,141, and Brit. 2,065, 116-A, the disclosures of which are herein incorporated by reference. Furthermore, the sulfonyl isocyanates of Formula IIa, which are disclosed in European Patent Pub. 44,212, may be prepared analogously to the teachings of U.S. Pat. No. 4,127,405. ##STR17## wherein R₈ and R₁₂ are as previously defined.

Certain compounds of Formula III are known in the art. For example, the compounds IIIa shown below: ##STR18## wherein X=CH₃, Cl or OCH₃ ; and

R₁ =CH₃ or C₂ H₅ ;

are described by W. Braker, et al., J. Amer. Chem. Soc., 69, 3072 (1947), the disclosures of which are herein incorporated by reference.

Triazines of Formula IIIb may be prepared according to the methods outlined in Equations 2 and 3. ##STR19## wherein R₁ and R₂ are as previously defined; and

Y is as defined in Equation 1, with m=0 or 2.

The reaction of Equation 2a is carried out according to the teachings of J. M. McElvain and R. L. Clarke, J. Amer. Chem. Soc., 69, 2657 (1947), in which the preparation of ethyl diethoxyiminoacetate is described. The intermediate N-cyanoimidates of Formula VI may be prepared according to the teaching of D. Lwowski in Synthesis, 1971, 263, by reacting V with cyanamide at pH 5.5, and these may be condensed according to reaction 2c with the appropriate compound of Formula VII in an alcoholic solvent at 25° to 80° C. to provide the appropriate triazines. Alternatively, the reaction of Equation 3a, described for substituted acetonitriles by F. C. Schaefer and G. A. Peters in J. Org. Chem., 26, 412 (1961), may be used to convert nitriles of Formula IV to the corresponding iminoesters. The free base may be carried on through reactions 2b or 2c, or, alternatively, converted to the amidinium hydrochloride salts (VIII) as described in the aforementioned reference. The compounds of Formula VIII may be converted to the compounds IIIb by the reaction of Equation 3c, in which VIII is contacted with a compound of Formula IX at 0° to 30° C. in the presence of 3-4 equivalents of the appropriate sodium alkoxide in the appropriate alcohol. The product may be isolated by evaporation of solvent, neutralization with aqueous acetic acid, and filtration. ##STR20## wherein Y is as defined in Equation 1 with m=0;

X is Rhd 1 or SCH₃ ; and

R₁ and R₂ are as previously defined.

The compounds of Formula IIIc may be prepared by the sequence of reactions outlined in Equation 4. ##STR21## wherein Y, m, R₁ and R₂ are as defined in Equation 3.

The reactions of Equations 4a and 4b are carried out as described by W. Braker, et al., loc. cit.

The compounds of Formula IIId may be prepared by similar methods shown in Equation 5. ##STR22## wherein R₂₁, R₁ and Y are as defined in Equation 1.

The reactions of Equations 5a and 5b are conducted as described for 2-amino-4-hydroxy-6-dimethoxymethylpyrimidine (J. I. De Graw and V. H. Brown, J. Het. Chem., 13, 439 (1976)). The silver salt of XIII may be prepared by addition of ammonia to an aqueous solution of XIII and an equivalent amount of silver nitrate. The dried silver salt may be contacted with one equivalent of methyl or ethyl iodide in a nonpolar solvent such as benzene at 25° to 80° C. to provide pyrimidines of Formula IIId after purification by column chromatography or recrystallization.

Alternatively, the compounds of Formula IIId may be prepared via the corresponding chloropyrimidines (IIIe). These may be obtained by the reaction of Equation 6a, in which a compound of Formula XIII is contacted with 2-5 equivalents of phosphorous oxychloride at 20°-90° C. for 3-30 hours. The product is isolated by removal of excess POCl₃ in vacuo, treatment of the residue with ice-water, extraction into an organic solvent, concentration, crystallization or column chromatography. The chloropyrimidines may then be converted to the compounds of Formula IIId by contacting with one equivalent of the appropriate sodium alkoxide in alcohol at 0°-30° C. followed by concentration and precipitation with ice-water. ##STR23## wherein Y is CH(QR₁)₂, CH₂ SR₁, CH(QR₂ Q), C(R₁)(QR₁)₂, CH(R₁)S(O)_(m) R₁ or C(R₁)(QR₂ Q);

R₁, R₂ and R₂₁ are as defined in Equation 1; and

m=0 or 2.

The ketoesters of Formula XII may be prepared by the methods of Equation 7. ##STR24## wherein m, Y and R₁ are as defined in Equation 3.

The reaction of Equation 7a is carried out by the slow addition of the appropriate dialkyl carbonate to a solution of the appropriate methyl ketone of Formula XV in an inert solvent (such as toluene) at 30°-110° in the presence of 1-2 equivalents of sodium hydride. The product may be isolated by concentration, neutralization, and extraction from water into an organic solvent, such as diethyl ether. The product may then be purified by distillation. Compounds of Formula XIIa may be obtained by the well-known reaction of a γ-chloroacetoacetic ester (XVI) with the appropriate sodium mercaptide or alkylsulfinate in a hydroxylic or dipolar aprotic solvent.

Cyclic acetals of Formula IIIe may be prepared from compounds of Formula IIIa according to Equation 8 by acetal exchange. ##STR25## wherein X, Q, Z, R₁ and R₂ are defined in Equation 1; and

R₂₂ is H, CH₃ or C₂ H₅.

The reaction of Equation 8 is carried out by heating the acyclic acetal in an inert solvent in the presence of one equivalent of a compound of Formula XVII and slightly more than one equivalent of an acidic catalyst, such as p-toluenesulfonic acid or boron trifluoride etherate with distillation of the by-product alcohol. The compound of Formula IIIe may be isolated by extraction with an organic solvent, and purified by crystallization or column chromatography.

The synthesis of N-methyl compounds of Formula IIIg may be accomplished by the procedure shown in Equation 9. ##STR26## wherein Z, R₁ and Q are as previously defined;

Y is as defined in Equation 1; and

X is CH₃, C₂ H₅, OCH₃ or OC₂ H₅.

The reaction of Equation 9a may be carried out by stirring a mixture of IIIf with one equivalent each of sodium hydride and dimethyl carbonate for 1-3 days in an inert solvent such as tetrahydrofuran or dimethylformamide. The product of Formula XVIII may be isolated by evaporation of solvent, neutralization with aqueous acetic acid, and filtration of the product. The reaction of Equation 8b is performed by adding XVI to a slurry of one equivalent of sodium hydride in tetrahydrofuran at 0°-30°, stirring for 1/2 hour, and adding methyl iodide, heating to reflux for 1-20 hours, and stirring with water and aqueous sodium hydroxide for 1-20 hours at 20°-30°. The product is isolated by evaporating the solvent, adding ice-water, and filtering.

The acetals and ketals of Formula IIIi may be prepared by the corresponding thioethers of Formula IIIh by the reaction of Equation 10. ##STR27## wherein X, R₁, R₂₁ and Z are as previously defined; and

R₂₂ is H, CH₃ or C₂ H₅.

The reaction of Equation 10 may be carried out by adding 2 to 2.3 equivalents of N-chlorosuccinimide to an alcoholic solution of a sulfide of Formula IIIh in the presence of 0.01 to 0.2 equivalents of a strong acid, such as H₂ SO₄, at -20° to 20° C. After 10 to 100 minutes, the reaction mixture is concentrated, diluted with water, and the reaction product is isolated by crystallization or extraction into an organic solvent.

Thioacetals and thioketals of Formula IIIj may be prepared by the reaction of Equation 11. ##STR28## wherein X is CH₃, C₂ H₅, OCH₃ or OC₂ H₅ ; and

Z, R₁, R₂₁ and R₂₂ are as defined in Equation 10.

The reaction of Equation 11a may be carried out by contacting a carbamate of Formula XVIIIa with 2-2.5 equivalents of lithium diisopropylamide in a solvent such as tetrahydrofuran at -78° and then with 1 to 2 equivalents of the appropriate dialkyl disulfide and allowing the mixture to warm to 20°. The product of Formula XVIIIb may be isolated by concentration, neutralization, and extraction into an organic solvent. Purification may be accomplished by column chromatrography or recrystallization. The reaction of Equation 11b is carried out by contacting with aqueous alkali for 10-100 minutes at 20°-80° and extracting the product into an organic solvent. The product may be isolated by concentration and crystallization.

The preparation of compounds of Formula IIIk is shown in Equation 12. ##STR29## wherein Z, R₁ and X are as defined in Equation 11.

The reaction of Equation 12a is carried out as described for Equation 11a, only using one equivalent of the appropriate alkyl iodide, rather than a disulfide. The reaction of Equation 12b is carried out as described for Equation 11b.

Sulfoxides and sulfones of Formula IIIl and IIIo, respectively, may be prepared from the corresponding sulfides of Formula IIIh as shown in Equation 13. ##STR30## wherein Z, X, R₁, R₂₁ and R₂₂ are as defined in Equation 10.

The reaction of Equation 13a is carried out by contacting IIIh with 0.9 to 1.1 equivalents of m-chloroperbenzoic acid in an inert solvent at -20° to 0° for 1 to 2 hours, concentration, and trituration with ether. If the product is ether-soluble, it is isolated by washing an ether solution with aqueous bicarbonate and concentration of the dried ether phase. The preparation of the corresponding sulfones is accomplished in the same way except that 2 to 2.2 equivalents of MCPBA are used at 0°-30° for 1-24 hours.

Compounds of Formula Ib may be prepared by acidic hydrolysis of compounds of Formula Ia according to Equation 14: ##STR31## wherein A, X, R₂₁ and Z are as defined in Equation 1.

The reaction of Equation 14 is carried out by stirring a solution or suspension of Ia in aqueous acetone containing a catalytic amount of a strong mineral acid, such as hydrochloric or sulfuric acid, at 0° to 30° C., followed by concentration and filtration of the product.

The compounds of Formula Ib may be in turn converted to compounds of Formulae Ic, Id, or Ie according to Equation 15: ##STR32## wherein A, X, Z, R₃, R₄, R₅, R₆ and R₂₁ are as previously defined.

The reactions of Equation 15 are carried out by contacting a compound of Formula Ib with at least one equivalent of an alkyl carboxylic anhydride, carbonyl chloride, chloroformate or carbamoyl chloride in an inert solvent in the presence of an excess of an acid acceptor such as pyridine, triethylamine, or aqueous sodium carbonate, followed by isolation of the product by acidification and crystallization or extraction into an organic solvent. Alternatively, compounds of Formula Ie wherein R₅ =H may be prepared by contacting the appropriate compound of Formula Ib with one equivalent of an appropriate alkyl isocyanate in an inert solvent and filtration of the product.

Certain compounds of Formula I may also be prepared by the reactions of Equation 16. ##STR33## wherein R₂₁, X and A are as previously defined, provided that R₇, R₁₆, R₁₈ and R₁₉ are not CO₂ R₉.

The reaction of Equation 16a is conducted in the same manner as described for Equation 1. The resulting compounds of Formula XIX may be converted to compounds of Formula If by contacting them with 3-5 equivalents of diisobutyl aluminum hydride in an ethereal solvent at -20° to 20°, after which the reaction mixture is quenched with aqueous mineral acid and extracted with an organic solvent. The product may be isolated by evaporation of solvent and crystallization.

Equation 17 outlines the preparation of the compounds of Formula XX. ##STR34## wherein R₁ and R₂₁ are as previously defined.

The pyrimidine of Formula XXII is described by Z. Budesinsky and F. Roubinek, in Coll. Czech. Chem. Comm., 26, 2871 (1961). This may be heated in an autoclave at 80° to 140° with ammonia or methyl amine to afford the amino acids of Formula XXIII. These may be esterified in the usual manner with methanol and acid, followed by evaporation of solvent, neutralization and filtration to afford the compounds of Formula XXa.

The preparation of XXb (R₂₁ =H) is reported in J. Org. Chem., 26, 2755, by G. Davies, et al., and the N-methyl compounds (R₂₁ =CH₃) may be prepared in an analogous fashion. The reaction of Equation 17c is conducted according to the procedure described for Equation 6b.

EXAMPLE 1 2-Amino-4-(dimethoxymethyl)-6-methylpyrimidine

To 6.9 g of sodium pellets in 120 ml of toluene containing 50 g of methyl dimethoxyacetate was added 20 g of acetone dropwise over 30 minutes at 0°-20°. The mixture was stirred overnight at room temperature, concentrated at reduced pressure, and the product was precipitated with ether and filtered. Ten ml of acetic acid in ice-water was added, and the β-diketone was extracted with methylene chloride. The residue from concentration of the organic extract was heated with 25 g of guanidine carbonate at 80°-90° for 30 minutes, cooled, digested with methylene chloride, filtered, dried with sodium sulfate, filtered, concentrated at reduced pressure, and triturated with petroleum ether to provide 11 g of 2-amino-4-dimethoxymethyl-6-methylpyrimidine, m.p. 69°-71° (lit, m.p. 71°-74°).

NMR (CDCl₃)δ: 2.3 (s, 3), 3.3 (s, 6), 5.0 (s, 1), 5.9 (br s, 2), 6.7 (s, 1).

EXAMPLE 2 2-Chloro-N-[[4-(dimethoxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]benzenesulfonamide

A solution of 0.3 g of 2-amino-4-dimethoxymethyl-6-methylpyrimidine in 50 ml of ether was stirred overnight at room temperature with 0.46 g of o-chlorobenzenesulfonyl isocyanate. The product was filtered and washed with hexane to provide 0.5 g of the title compound, m.p. 150°-153°.

NMR (CDCl₃)δ: 2.5 (s, 3), 3.4 (s, 6), 5.2 (s, 1), 7.1 (s, 1), 7.4 (m, 3), 7.9 (br s, 1), 8.3 (m, 1).

EXAMPLE 3 2-Amino-4-methyl-6-(tetrahydrofuran-2-yloxymethyl)-pyrimidine

A solution containing 30 g of methyl glycolate, 33 g of dihydropyran, and 0.2 g of p-toluenesulfonic acid in 100 ml of toluene was stirred at room temperature overnight. After cooling at -5°, 6.8 g of sodium pellets was added, followed by 24 ml of acetone at -5° to 8°. Stirring was continued for 20 hours at room temperature, after which time hexane was added, and the solution was poured into ice-water and partitioned. The aqueous phase was washed with ether and acidified with 20 ml of acetic acid, extracted with 600 ml of methylene chloride, the organic layer was dried (MgSO₄) and concentrated, and the residue was heated at 80°-90° with 28 g of guanidine carbonate for 1 hour. Addition of ice-water to the cooled reaction mixture precipitated the product, which was filtered and dried to afford the title compound, m.p. 109°-110.5°.

NMR (CDCl₃)δ: 1.7 (br s, 6), 2.3 (s, 3), 3.6 (br m, 2), 4.5 (d, 2), 4.7 (m, 1), 5.4 (br s, 2), 6.6 (br s, 1).

EXAMPLE 4 Methyl 2-[[[4-methyl-6-(tetrahydropyran-2-yloxymethyl)-pyrimidin-2yl]aminocarbonyl]aminosulfonyl]benzoate

To a solution of 3.25 g of the product from Example 3 in 50 ml of ether was added 3.75 g of 2-methoxycarbonylbenzenesulfonyl isocyanate and the mixture was stirred for 3 hours under nitrogen. The precipitated product was filtered and washed with ether to afford 6.0 g of the title compound, m.p. 126°-128°(d).

EXAMPLE 5 Methyl [[[4-(hydroxymethyl)-6-methylpyrimidin-2-yl]-aminocarbonyl]aminosulfonyl]benzoate

A solution of 6 g of the product prepared in Example 4 in 50 ml of acetone was stirred with 3 ml of 1N aqueous HCl for 3 days at room temperature, concentrated at reduced pressure, and the residue was thoroughly washed with water to provide 4 g of the title compound, m.p. 140°-141°.

NMR (CDCl₃ +DMSO-d₆)δ: 2.5 (s, 3), 3.9 (s, 3), 4.6 (br s, 2), 7.0 (br s, 1), 7.6 (m, 3 ), 8.3 (m, 1), 9.6 (br s, 1).

EXAMPLE 6 Methyl [[[4-(acetoxymethyl)-6-methylpyrimidin-2-yl]-aminocarbonyl]aminosulfonyl]benzoate

To 0.5 g of the compound from Example 5 was added 1 ml of acetic anhydride and 1 ml of pyridine. After 1 hour at room temperature, ice-water was added, the precipitated oil was triturated, filtered, and washed with water to afford 0.4 g of the title compound, m.p. 145°-150°.

NMR (CDCl₃)δ: 2.2 (s, 3), 2.6 (s, 3), 3.9 (s, 3), 5.2 (s, 2), 6.9 (s, 1), 7.7 (m, 3), 8.3 (br s, 1), 8.4 (m, 1), 13.1 (br s, 1).

                                      TABLE 1a                                     __________________________________________________________________________      ##STR35##                                                                     R.sub.7   R.sub.8                                                                             R.sub.21                                                                          X    Y        m.p. (° C.)                             __________________________________________________________________________     Cl        H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     150-153°                                CO.sub.2 CH.sub.3                                                                        H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     121-125°                                SO.sub.2 CH.sub.3                                                                        H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     152-155°                                NO.sub.2  H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     144-152°                                CO.sub.2 CH(CH.sub.3).sub.2                                                              H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                      73-79°                                 CO.sub.2 C.sub.2 H.sub.5                                                                 H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CF.sub.3  H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Br        H    H  CH.sub.3                                                                            CH(OCH.sub.3 ).sub.2                                    CH.sub.3  H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     C.sub.2 H.sub.5                                                                          H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 -n-C.sub.3 H.sub.7                                                              H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     135-145° d                              SO.sub.2 N(CH.sub.3).sub.2                                                               H    H  CH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                                                     146-157°                                OCH.sub.3 6-OCHF.sub.2                                                                        H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OCF.sub.2 CF.sub.2 H                                                                     H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH.sub.2 OCH.sub.3                                                                       H    H  CH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     OSO.sub.2 CHCl.sub.2                                                                     H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SC.sub.2 H.sub.5                                                                         H    H  CH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     OSO.sub.2 CH.sub.3                                                                       H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OSO.sub.2 C.sub.2 H.sub.5                                                                H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                     H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 C.sub.2 H.sub.5                                                                 H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     NO.sub.2  5-CF.sub.3                                                                          H  CH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     SO.sub.2 -n-C.sub.3 H.sub.7                                                              3-Cl H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OC.sub.2 H.sub.5                                                                         5-NO.sub.2                                                                          H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 C.sub.2 H.sub.5                                                                 H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                      98-100° d                              I         H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                      6-NO.sub.2                                                                          H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Cl        5-Cl H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                        5-Cl H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.3                                                                        4-F  H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OCH.sub.2 CHCH.sub.2                                                                     H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH(OCH.sub.3)CH.sub.3                                                                    H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 CF.sub.3                                                                        H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SCHF.sub.2                                                                               H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OCH.sub.2 CHCHCH.sub.3                                                                   H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Cl        H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.3                                                                        H    CH.sub.3                                                                          CH.sub. 3                                                                           CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CH.sub.3                                                               H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                        H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 N(CH.sub.3).sub.2                                                               H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH(CH.sub.3).sub.2                                                                       H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OCH.sub.3 H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SCH.sub.3 H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 -n-C.sub.3 H.sub.7                                                              H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      -n-C.sub.4 H.sub.9                                                                      H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     O -n-C.sub.4 H.sub.9                                                                     H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     NO.sub.2  H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 -n-C.sub.4 H.sub.9                                                              H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Cl        H    H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            CH.sub.2 OCH.sub.3                                                                       H    H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            SO.sub.2 C.sub.2 H.sub.5                                                                 H    H  CH.sub. 3                                                                           C(CH.sub.3)(OCH.sub.3).sub.2                            OCH.sub.3 H    H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            SC.sub.2 H.sub.5                                                                         H    H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            CO.sub.2 C.sub.2 H.sub.5                                                                 H    H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            CO.sub.2 CH.sub.3                                                                        5-Cl H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            Cl        H    H  CH.sub.3                                                                            CH(SCH.sub.3).sub.2                                     CO.sub.2 CH.sub.3                                                                        H    H  CH.sub.3                                                                            CH(SCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                        H    H  CH.sub.3                                                                            CH(SCH.sub.3).sub.2                                     NO.sub.2  H    H  CH.sub.3                                                                            CH(SCH.sub.3).sub.2                                     __________________________________________________________________________

                  TABLE 1b                                                         ______________________________________                                          ##STR36##                                                                                                               m.p.                                 R.sub.7     R.sub.8 R.sub.21                                                                              X      Y       (° C.)                        ______________________________________                                         NO.sub.2    H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                                                          129-                                                                           132°                          Br          H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                Cl          H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                                                          148-                                                                           150°                          SO.sub.2 CH.sub.3                                                                          H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                                                          161-                                                                           165°                          F           H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                H           H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                CO.sub.2 CH.sub.3                                                                          H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                                                          126-                                                                           128°                          CH.sub. 3   5-      H      CH.sub.3                                                                              CH.sub.2 OTHP                                            SCHF.sub.2                                                         SO.sub.2 N(CH.sub.3).sub.2                                                                 H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                SO.sub.2 -n-C.sub.3 H.sub.7                                                                H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                OCH.sub.3   H       H      CH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                O -n-C.sub.3 H.sub.7                                                                       H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                CH.sub.2 OCH.sub.3                                                                         H       H      CH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                SO.sub.2 N(CH.sub.3).sub.2                                                                 H       CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.2 OTHP                                OC.sub.2 H.sub.5                                                                           H       CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.2 OTHP                                CO.sub.2 Et H       CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.2 OTHP                                OCF.sub.2 CF.sub.2 H                                                                       H       CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.2 OTHP                                CH.sub.2 OCH.sub.3                                                                         H       CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.2 OTHP                                Cl          H       CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.2 OTHP                                SC.sub.2 H.sub.5                                                                           H       CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.2 OTHP                                SO.sub.2 CH.sub.2 CHCH.sub.2                                                               H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                SCF.sub.3   H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                CH(OCH.sub. 3)CH.sub.3                                                                     H       H      CH.sub.3                                                                              CH.sub.2 OTHP                                ______________________________________                                    

                                      TABLE 1c                                     __________________________________________________________________________      ##STR37##                                                                     R.sub.7     R.sub.8                                                                              R.sub.21                                                                           X     Y     m.p. (° C.)                           __________________________________________________________________________     Cl          H     H   CH.sub.3                                                                             CH.sub.2 OH                                                                          130-132°                              CO.sub.2 CH.sub.3                                                                          H     H   CH.sub.3                                                                             CH.sub.2 OH                                                                          140-141°                              SO.sub.2 CH.sub.3                                                                          H     H   CH.sub.3                                                                             CH.sub.2 OH                                                                          155° d                                NO.sub.2    H     H   CH.sub.3                                                                             CH.sub.2 OH                                                                          112-116°                              CO.sub.2 CH(CH.sub.3).sub.2                                                                H     H   CH.sub.3                                                                             CH.sub.2 OH                                                                          154-157°                              CO.sub.2 C.sub.2 H.sub.5                                                                   H     H   CH.sub.3                                                                             CH.sub.2 OH                                        CF.sub.3    H     H   CH.sub.2 CH.sub.3                                                                    CH.sub.2 OH                                        Br          H     H   CH.sub.3                                                                             CH.sub.2 OH                                        CH.sub.3    H     H   CH.sub.3                                                                             CH.sub.2 OH                                        C.sub.2 H.sub.5                                                                            H     H   CH.sub.3                                                                             CH.sub.2 OH                                        SO.sub.2 -n-C.sub.3 H.sub.7                                                                H     H   CH.sub.3                                                                             CH.sub.2 OH                                                                          128° d                                SO.sub.2 N(CH.sub.3).sub.2                                                                 H     H   CH.sub.3                                                                             CH.sub.2 OH                                                                          163-169° d                            OCH.sub.3   H     H   CH.sub.3                                                                             CH.sub.2 OH                                        CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H     H   CH.sub.3                                                                             CH.sub.2 OH                                        OCF.sub.2 CF.sub.2 H                                                                       H     H   CH.sub.3                                                                             CH.sub.2 OH                                        CH.sub.2 OCH.sub.3                                                                         H     H   CH.sub.3                                                                             CH.sub.2 OH                                        OSO.sub.2 CHCl.sub.2                                                                       H     H   CH.sub.3                                                                             CH.sub.2 OH                                        SC.sub.2 H.sub.5                                                                           H     H   CH.sub.3                                                                             CH.sub.2 OH                                        OSO.sub.2 CH.sub.3                                                                         3-OCHF.sub.2                                                                         H   CH.sub.3                                                                             CH.sub.2 OH                                        OSO.sub.2 C.sub.2 H.sub.5                                                                  H     H   CH.sub.3                                                                             CH.sub.2 OH                                        CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                       H     H   CH.sub.3                                                                             CH.sub.2 OH                                        SO.sub.2 C.sub.2 H.sub.5                                                                   H     H   CH.sub.2 CH.sub.3                                                                    CH.sub.2 OH                                        NO.sub.2    5-CF.sub.3                                                                           H   CH.sub.3                                                                             CH.sub.2 OH                                        SO.sub.2 -n-C.sub.3 H.sub.7                                                                3-Cl  H   CH.sub.3                                                                             CH.sub.2 OH                                        OC.sub.2 H.sub.5                                                                           5-NO.sub.2                                                                           H   CH.sub.3                                                                             CH.sub.2 OH                                        SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        6-NO.sub.2                                                                           H   CH.sub.3                                                                             CH.sub.2 OH                                        Cl          5-Cl  H   CH.sub.3                                                                             CH.sub.2 OH                                        SO.sub.2 CH.sub.3                                                                          5-Cl  H   CH.sub.2 CH.sub.3                                                                    CH.sub.2 OH                                        CO.sub.2 CH.sub.3                                                                          4-F   H   CH.sub.3                                                                             CH.sub.2 OH                                        NO.sub.2    H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        Br          H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        Cl          H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        SO.sub.2 CH.sub.3                                                                          H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        F           H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        H           H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        CO.sub.2 CH.sub.3                                                                          H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        CH.sub.3    H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        SO.sub.2 -i-C.sub.3 H.sub.7                                                                H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        SCF.sub.3   H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        SO.sub.2 CH.sub.2 CHCH.sub.2                                                               H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        SCH.sub.2 CH.sub.3                                                                         H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        OCH.sub. 2 CHCH.sub.2                                                                      H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        OCH.sub.2 C(CH.sub.3)CH.sub.2                                                              H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        CH.sub.2 OEt                                                                               H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        CH(OCH.sub.3)CH.sub.3                                                                      H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                              H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        O- -i-C.sub.3 H.sub.7                                                                      H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                         -i-C.sub.4 H.sub.9                                                                        H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                        SO.sub.2 Et H     H   CH.sub.3                                                                             CH.sub.2 OH                                         -n-C.sub.4 H.sub.9                                                                        H     H   CH.sub.3                                                                             CH.sub.2 OH                                        O -n-C.sub.4 H.sub.9                                                                       H     H   CH.sub.3                                                                             CH.sub.2 OH                                        O -t-C.sub.4 H.sub.9                                                                       H     H   CH.sub.3                                                                             CH.sub.2 OH                                        SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        H     H   CH.sub.3                                                                             CH.sub.2 OH                                        I           H     H   CH.sub.3                                                                             CH.sub.2 OH                                        OCF.sub.2 H H     H   CH.sub.3                                                                             CH.sub.2 OH                                        SCF.sub.2 CF.sub.2 H                                                                       H     H   CH.sub.3                                                                             CH.sub.2 OH                                        CH.sub.2 Cl H     H   CH.sub.3                                                                             CH.sub.2 OH                                        __________________________________________________________________________

                                      TABLE 1d                                     __________________________________________________________________________      ##STR38##                                                                     R.sub.7   R.sub.8                                                                               R.sub.21                                                                          X  Y            m.p. (° C.)                         __________________________________________________________________________     H         H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                H         H      H  CH.sub.3                                                                          CH(OEt).sub.2                                           H         H      H  C.sub.2 H.sub.5                                                                   CH.sub.2 OCOCH.sub.3                                    H         H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                      H         H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       Cl        H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    158-163°                            Cl        H      CH.sub.3                                                                          CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                Cl        H      H  C.sub.2 H.sub.5                                                                   CH(OCH.sub.2 CH.sub.2 O)                                Cl        H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       Cl        6-Cl   H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       Cl        H      CH.sub.3                                                                          CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       Cl        4-F    H  CH.sub.3                                                                          CH(OEt).sub.2                                           Cl        H      H  CH.sub.3                                                                          CH(OEt).sub.2                                           CH.sub.3  H      H  CH.sub.3                                                                          CH(OEt).sub.2                                           CH.sub.3  H      H  C.sub.2 H.sub.5                                                                   CH(OEt).sub.2                                           CH.sub.3  H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                      C.sub.2 H.sub.5                                                                          H      H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    C.sub.2 H.sub.5                                                                          H      CH.sub.3                                                                          CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    C.sub.2 H.sub.5                                                                          5-Cl   H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                     -n-C.sub.4 H.sub.9                                                                      H      H  CH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                             OCH.sub.3 H      H  CH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                             OCH.sub.3 3-NO.sub.2                                                                            H  CH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                             OCH.sub.3 H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                OCH.sub.3 H      H  CH.sub.3                                                                          CH(OEt).sub.2                                           OSO.sub.2 CH.sub.3                                                                       H      H  CH.sub.3                                                                          CH(CH.sub.3)SCH.sub.3                                                                       151-155°                            CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH(CH.sub.3)SCH.sub.3                                                                       153-157°                            SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH(CH.sub.3)SCH.sub. 3                                                                      104-107°                            NO.sub.2  H      H  CH.sub.3                                                                          CH(CH.sub.3)SCH.sub.3                                                                       133-138°                            CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                                                        145-150°                            CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                       CO.sub.2 CH.sub.3                                                                        H      H  C.sub.2 H.sub.5                                                                   CH(OEt).sub.2                                           CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH.sub.2 SEt                                            CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    151-156°                            CO.sub.2 CH.sub.3                                                                        H      CH.sub.3                                                                          CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CO.sub.2 CH.sub.3                                                                        6-CH.sub.3                                                                            H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CO.sub.2 CH.sub.3                                                                        5-OEt  H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CO.sub.2 CH.sub.3                                                                        4-CF.sub.3                                                                            H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH.sub.2 OCOEt                                          SO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH.sub.2 OCOEt                                          SO.sub.2 CH.sub.3                                                                        3-F    H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                      SO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    193-195° d                          SO.sub.2 CH.sub.3                                                                        H      CH.sub.3                                                                          CH.sub. 3                                                                         CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 CH.sub.3                                                                        6-O -n-C.sub.3 H.sub.7                                                                H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 CH.sub.3                                                                        3- -i-C.sub.3 H.sub.7                                                                 H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH.sub.2 OCO -n-C.sub.3 H.sub.7                         SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH(SCH(CH.sub.3)CH.sub.2 S)                             SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    185-187°                            SO.sub.2 N(CH.sub.3).sub.2                                                               H      CH.sub.3                                                                          CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 N(CH.sub.3).sub.2                                                               6-NO.sub.2                                                                            H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                NO.sub.2  3-Br   H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                NO.sub.2  6-Cl   CH.sub.3                                                                          CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                NO.sub.2  H      H  C.sub.2 H.sub.5                                                                   CH(OCH.sub.2 CH.sub.2 O)                                NO.sub.2  H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    179-182° d                          NO.sub.2  3-F    H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       Br        H      H  CH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 S)                                Br        H      H  CH.sub.3                                                                          CH.sub.2 OCO.sub.2 CH.sub.3                             CO.sub.2 CH.sub.2 CH.sub.3                                                               H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    119-121°                            I         H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CH.sub.2 Cl                                                                              H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                OCHF.sub.2                                                                               H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                Br        H      CH.sub.3                                                                          CH.sub.3                                                                          CH.sub.2 OCONHCH.sub.3                                  CF.sub.3  H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                CF.sub.3  H      H  CH.sub.3                                                                          CH.sub.2 SEt                                            SO.sub.2 N(Et).sub.2                                                                     H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                OCH.sub.2 CH.sub.3                                                                       H      H  C.sub.2 H.sub.5                                                                   CH(OCH.sub.2 CH.sub.2 O)                                O -n-C.sub.4 H.sub.9                                                                     H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                O -i-C.sub.3 H.sub.7                                                                     H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                OCH.sub.2 CHCH.sub.2                                                                     H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 CF.sub.3                                                                        H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 CF.sub.3                                                                        5-CF.sub.3                                                                            H  CH.sub.3                                                                          CH(OEt).sub.2                                           SO.sub.2 CF.sub.3                                                                        H      H  CH.sub.3                                                                          CH(OEt).sub.2                                           SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      H  CH.sub.3                                                                          CH(OEt).sub.2                                           SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      CH.sub.3                                                                          CH.sub.3                                                                          CH(OEt).sub.2                                           SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                    144° d                              OCF.sub.2 CF.sub.2 H                                                                     H      H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    OCF.sub.2 CF.sub.2 H                                                                     H      H  C.sub.2 H.sub.5                                                                   CH.sub.2 OCOCH.sub.3                                    OCF.sub.2 CF.sub.2 H                                                                     H      H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    OSO.sub.2 C.sub.2 H.sub.5                                                                H      H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    CH.sub.2 OEt                                                                             6-F    H  CH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                            H      H  CH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                             SO.sub.2 N(CH.sub.3)Et                                                                   H      H  CH.sub.3                                                                          CH.sub.2 OCO.sub.2 Et                                   SO.sub.2 N(CH.sub.3)Et                                                                   H      H  CH.sub.3                                                                          CH.sub.2 OCON(CH.sub.3).sub.2                           SO.sub.2 N(CH.sub.3)Et                                                                   H      H  CH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       Cl        H      H  CH.sub.3                                                                          CH(SEt).sub.2                                           CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          C(CH.sub.3)(SCH.sub.3).sub.2                            CO.sub.2 C.sub.2 H.sub.5                                                                 H      H  CH.sub.3                                                                          C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                       NO.sub.2  H      H  CH.sub.3                                                                          C(C.sub.2 H.sub.5)(SCH.sub.2 CH.sub.2 CH.sub.2 S)       SO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH(CH.sub.3)SO.sub.2 CH.sub.3                           SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                          179-185°                            CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                          133-138°                            Cl        H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                          133-135°                            NO.sub.2  H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                          148-154°                            SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                          127-133°                            Cl        H      H  CH.sub.3                                                                          CH.sub.2 SO.sub.2 CH.sub.3                                                                  182-187°                            Cl        H      H  CH.sub.3                                                                          CH.sub.2 S(O)CH.sub.3                                   SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  CH.sub.3                                                                          CH(CH.sub.3)(S(O)CH.sub.3)                              NO.sub.2  H      H  CH.sub.3                                                                          CH(CH.sub.3)(SO.sub.2 CH.sub.3)                         Cl        H      H  CH.sub.3                                                                          CH.sub.2 S(O)CH.sub.2 CH.sub.3                          CO.sub.2 CH.sub.3                                                                        H      H  CH.sub.3                                                                          CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                     SO.sub.2 CH.sub.2 CH.sub.3                                                               H      H  CH.sub.3                                                                          CH.sub.2 S(O)CH.sub.3                                   __________________________________________________________________________

                                      TABLE 1e                                     __________________________________________________________________________      ##STR39##                                                                     R.sub.7   R.sub.8                                                                            R.sub.21                                                                          X     Y        m.p. (°C.)                              __________________________________________________________________________     Cl        H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     179-182°                                CO.sub.2 CH.sub.3                                                                        H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     121-131°                                SO.sub.2 CH.sub.3                                                                        H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     162° d                                  NO.sub.2  H   H  OCH   CH(OCH.sub.3).sub.2                                                                     150° d                                  CO.sub.2 CH(CH.sub.3).sub.2                                                              H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 C.sub.2 H.sub.5                                                                 H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CF.sub.3  H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Br        H   CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH.sub.3  H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     C.sub.2 H.sub.5                                                                          H   H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     SO.sub.2 -n-C.sub.3 H.sub.7                                                              H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     161-167° d                              SO.sub.2 N(CH.sub.3).sub.2                                                               H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                      93-102° d                              OCH.sub.3 H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OCF.sub.2 CF.sub.2 H                                                                     H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH.sub.2 OCH.sub.3                                                                       H   H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     OSO.sub.2 CHCl.sub.2                                                                     H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SC.sub.2 H.sub.5                                                                         H   CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OSO.sub.2 CH.sub.3                                                                       H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OSO.sub.2 C.sub.2 H.sub.5                                                                H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                     H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 C.sub.2 H.sub.5                                                                 H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     NO.sub.2  5-CF.sub.3                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 -n-C.sub.3 H.sub.7                                                              3-Cl                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OC.sub.2 H.sub.5                                                                         5-NO.sub.2                                                                         H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     OSO.sub.2 CH.sub.3                                                                       H   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            CO.sub.2 CH.sub.3                                                                        H   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            CO.sub.2 CH.sub.2 CH.sub.3                                                               H   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                      6-NO.sub.2                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Cl        5-Cl                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                        5-Cl                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.3                                                                        4-F H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     __________________________________________________________________________

                  TABLE 1f                                                         ______________________________________                                          ##STR40##                                                                                                               m.p.                                 R.sub.7      R.sub.8                                                                               R.sub.21                                                                              X      Y       (°C.)                         ______________________________________                                         NO.sub.2     H      H      OCH.sub.3                                                                             CH.sub.2 OTHP                                Br           H      H      OCH.sub.3                                                                             CH.sub.2 OTHP                                Cl           H      H      OCH.sub.3                                                                             CH.sub.2 OTHP                                SO.sub.2 CH.sub.3                                                                           H      H      OCH.sub.3                                                                             CH.sub.2 OTHP                                F            H      H      OCH.sub.3                                                                             CH.sub.2 OTHP                                H            H      H      OCH.sub.3                                                                             CH.sub.2 OTHP                                CO.sub.2 CH.sub.3                                                                           H      H      OCH.sub.3                                                                             CH.sub.2 OTHP                                CH.sub.3     H      H      OCH.sub.3                                                                             CH.sub.2 OTHP                                SO.sub.2 N(CH.sub.3).sub.2                                                                  H      H      OCH.sub.3                                                                             CH.sub.2 OTHP                                SO.sub.2 -n-C.sub.3 H.sub.7                                                                 H      H      OCH.sub. 3                                                                            CH.sub.2 OTHP                                OCH.sub.3    H      H      OCH.sub.3                                                                             CH.sub.2 OTHP                                O -n-C.sub.3 H.sub.7                                                                        H      CH.sub.3                                                                              OCH.sub.3                                                                             CH.sub.2 OTHP                                CH.sub.2 OCH.sub.3                                                                          H      CH.sub.3                                                                              OCH.sub.3                                                                             CH.sub.2 OTHP                                CO.sub.2 CH.sub.2 CHCH.sub.2                                                                H      H      OCH.sub.3                                                                             CH.sub.2 OTHP                                Cl           6-Cl   H      OCH.sub.3                                                                             CH.sub.2 OTHP                                I            H      H      OCH.sub.3                                                                             CH.sub.2 OTHP                                ______________________________________                                    

                  TABLE 1g                                                         ______________________________________                                          ##STR41##                                                                                                        m.p.                                        R.sub.7     R.sub.8 R.sub.21                                                                              X       Y(°C.)                               ______________________________________                                         Cl          H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH.sub.3                                                                          H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                          H       H      OCH.sub.3                                                                              CH.sub.2 OH 170° d                   NO.sub.2    H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                                H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 C.sub.2 H.sub.5                                                                   H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CF.sub.3    H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 Br          H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CH.sub.3    H       CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                                 C.sub.2 H.sub.5                                                                            H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                                H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                                 H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 OCH.sub.3   H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H       H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 OCF.sub.2 CF.sub.2 H                                                                       H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CH.sub.2 OCH.sub.3                                                                         H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 OSO.sub.2 CHCl.sub.2                                                                       H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 SC.sub.2 H.sub.5                                                                           H       CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                                 OSO.sub.2 CH.sub.3                                                                         H       H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 OSO.sub.2 C.sub.2 H.sub.5                                                                  H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                       H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 C.sub.2 H.sub.5                                                                   H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 NO.sub.2    5-CF.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                                3-Cl    H      OCH.sub.3                                                                              CH.sub.2 OH                                 OC.sub.2 H.sub.5                                                                           5-NO.sub.2                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 I           H       H      OCH.sub.3                                                                              CH.sub. 2 OH                                SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        6-NO.sub.2                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 Cl          5-Cl    H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                          5-Cl    H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH.sub.3                                                                          4-F     H      OCH.sub.3                                                                              CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 1h                                     __________________________________________________________________________      ##STR42##                                                                     R.sub.7   R.sub.8                                                                               R.sub.21                                                                          X   Y           m.p. (°C.)                          __________________________________________________________________________     H         H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               H         H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                          H         H      H  OC.sub.2 H.sub.5                                                                   CH.sub.2 OCOCH.sub.3                                   H         H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                     H         H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      Cl        H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   105-112° d                          Cl        H      CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               Cl        H      H  OC.sub.2 H.sub.5                                                                   CH(OCH.sub.2 CH.sub.2 O)                               Cl        H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      Cl        6-Cl   H  OCH.sub.3                                                                          OCH(OCH.sub. 2 CH.sub.2 CH.sub.2 O)                    Cl        H      CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      Cl        4-F    H  OCH.sub.3                                                                          CH(OEt).sub.2                                          Cl        H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                                                              143-145°                            CH.sub.3  H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                          CH.sub.3  H      H  OC.sub.2 H.sub.5                                                                   CH(OEt).sub.2                                          CH.sub.3  H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                     C.sub.2 H.sub.5                                                                          H      H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   C.sub.2 H.sub.5                                                                          H      CH.sub.3                                                                          OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   C.sub.2 H.sub.5                                                                          5-Cl   H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                    -n-C.sub.4 H.sub.9                                                                      H      H  OCH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                            OCH.sub.3 H      H  OCH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                            OCH.sub.3 3-NO.sub.2                                                                            H  OCH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                            OCH.sub.3 H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               OCH.sub.3 H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                          CO.sub.2 CH.sub.2 CH.sub.3                                                               H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   145-149°                            Cl        H      H  OCH.sub.3                                                                          C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                      CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub. 3                                                                         C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                      C.sub.2 H.sub.5                                                                          H      H  OCH.sub.3                                                                          C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                      SO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                      CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                      CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                                                              127-144°                            CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 SEt                                           CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   161-163°                            CO.sub.2 CH.sub.3                                                                        H      CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               CO.sub.2 CH.sub.3                                                                        6-CH.sub.3                                                                            H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               CO.sub.2 CH.sub.3                                                                        5-OEt  H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               CO.sub.2 CH.sub.3                                                                        4-CF.sub.3                                                                            H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 OCOEt                                         SO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                                                              210-213°                            SO.sub.2 CH.sub.3                                                                        3-F    H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                     SO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 CH.sub.3                                                                        H      CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 CH.sub.3                                                                        6-O -n-C.sub.3 H.sub.7                                                                H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 CH.sub.3                                                                        3- .sub.-i-C.sub.3 H.sub.7                                                            H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          CH.sub.2 OCO -n-C.sub.3 H.sub.7                        SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                                                              138-141°                            SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          CH(SCH(CH.sub.3)CH.sub.2 S)                            SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 N(CH.sub.3).sub.2                                                               H      CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 N(CH.sub.3).sub.2                                                               6-NO.sub.2                                                                            H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               NO.sub.2  3-Br   H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               NO.sub.2  6-Cl   CH.sub.3                                                                          OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               NO.sub.2  H      H  OC.sub.2 H.sub.5                                                                   CH(OCH.sub.2 CH.sub.2 O)                               NO.sub.2  H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               NO.sub.2  3-F    H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      Br        H      H  OCH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 S)                               Br        H      H  OCH.sub.3                                                                          CH.sub.2 OCO.sub.2 CH.sub.3                            CO.sub.2 C.sub.2 H.sub.5                                                                 H      H  OCH.sub.3                                                                          CH(CH.sub.3)SC.sub.2 H.sub.5                           Br        H      H  OCH.sub.3                                                                          CH(CH.sub.2 CH.sub.3)SCH.sub.3                         SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          C(CH.sub.3)(SCH.sub.2 CH.sub.2 S)                      CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(SCH.sub.3).sub.2                                    Br        H      CH.sub.3                                                                          OCH.sub.3                                                                          CH.sub.2 OCONHCH.sub.3                                 CF.sub.3  H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               CF.sub.3  H      H  OCH.sub.3                                                                          CH.sub.2 SEt                                           SO.sub.2 N(Et).sub.2                                                                     H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               OCH.sub.2 CH.sub.3                                                                       H      H  OC.sub.2 H.sub.5                                                                   CH(OCH.sub.2 CH.sub.2 O)                               O -n-C.sub.4 H.sub.9                                                                     H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               O .sub.-i-C.sub.3 H.sub.7                                                                H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               OCH.sub.2 CHCH.sub.2                                                                     H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 CF.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               SO.sub.2 CF.sub.3                                                                        5-CF.sub.3                                                                            H  OCH.sub.3                                                                          CH(OEt).sub.2                                          SO.sub.2 CF.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                          SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      H  OCH.sub.3                                                                          CH(OEt).sub.2                                          SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      CH.sub.3                                                                          OCH.sub.3                                                                          CH(OEt).sub.2                                          SO.sub.2 -n-C.sub.3 H.sub.7                                                              H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                               OCF.sub.2 CF.sub.2 H                                                                     H      H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   OCF.sub.2 CF.sub.2 H                                                                     H      H  OC.sub.2 H.sub.5                                                                   CH.sub.2 OCOCH.sub.3                                   OCF.sub.2 CF.sub.2 H                                                                     H      H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   OSO.sub.2 C.sub.2 H.sub.5                                                                H      H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   CH.sub.2 OEt                                                                             6-F    H  OCH.sub.3                                                                          CH.sub.2 OCOCH.sub.3                                   CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                            H      H  OCH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                            SO.sub.2 N(CH.sub.3)Et                                                                   H      H  OCH.sub.3                                                                          CH.sub.2 OCO.sub.2 Et                                  SO.sub.2 N(CH.sub.3)Et                                                                   H      H  OCH.sub.3                                                                          CH.sub.2 OCON(CH.sub.3).sub.2                          SO.sub.2 N(CH.sub.3)Et                                                                   H      H  OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      Cl        H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         149-152°                            CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         146-149°                            CO.sub.2 CH.sub.2 CH.sub.3                                                               H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         146-149°                            SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         136-146° d                          NO.sub.2  H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         152-156° d                          SO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         185-188°                            Cl        H      H  OCH.sub.3                                                                          CH.sub.2 SO.sub.2 CH.sub.3                                                                 158-158.5°                          CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 SO.sub.2 CH.sub.3                                                                 58° d                               Cl        H      H  OCH.sub.3                                                                          CH(CH.sub.3)(S(O)CH.sub.3)                             CO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH(CH.sub.3)(SO.sub. 2 CH.sub.3)                       CO.sub.2 CH.sub.2 CH.sub.3                                                               H      H  OCH.sub.3                                                                          CH.sub.2 S(O)CH.sub.3                                  SO.sub.2 N(CH.sub.3).sub.2                                                               H      H  OCH.sub.3                                                                          CH.sub.2 S(O)CH.sub.2 CH.sub.3                         NO.sub.2  6-Cl   H  OCH.sub.3                                                                          CH.sub.2 S(O)CH.sub.3                                  SO.sub.2 CH.sub.3                                                                        H      H  OCH.sub.3                                                                          CH.sub.2 S(O)CH.sub.3                                  Cl        H      H  OCH.sub.3                                                                          CH(CH.sub.3)(S(O)CH.sub.2 CH.sub.3)                    __________________________________________________________________________

                  TABLE 1i                                                         ______________________________________                                          ##STR43##                                                                                                               m.p.                                 R.sub.7     R.sub.8 R.sub.21                                                                              X   Y          (°C.)                         ______________________________________                                         Cl          H       H      Cl  CH(OCH.sub.3 .sub.)2                                                                      164-                                                                           166°                          CO.sub.2 CH.sub.3                                                                          H       H      Cl  CH(OCH.sub.3).sub.2                                                                       149-                                                                           152°                          SO.sub.2 CH.sub.3                                                                          H       H      Cl  CH(OCH.sub.3).sub.2                             NO.sub.2    H       H      Cl  CH(OC.sub.2 H.sub.5).sub.2                      CO.sub.2 CH(CH.sub.3).sub.2                                                                H       H      Cl  CH.sub.2 SCH.sub.3                              CO.sub.2 C.sub.2 H.sub.5                                                                   H       CH.sub.3                                                                              Cl  CH.sub.2 SC.sub.2 H.sub.5                       CF.sub.3    H       H      Cl  CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)               Br          H       H      Cl  CH(OCH.sub.3).sub.2                             CH.sub.3    H       H      Cl  CH(OCH.sub.3).sub.2                             C.sub.2 H.sub. 5                                                                           H       H      Cl  CH(OCH.sub.3).sub.2                             SO.sub.2 -n-C.sub.3 H.sub.7                                                                H       H      Cl  CH(OCH.sub.3).sub.2                             SO.sub.2 N(CH.sub.3).sub.2                                                                 H       H      Cl  CH(OCH.sub.3).sub.2                             OCH.sub.3   H       CH.sub.3                                                                              Cl  CH(OCH.sub.3).sub.2                             CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H       H      Cl  CH(OCH.sub.3).sub.2                             OCF.sub.2 CF.sub.2 H                                                                       H       H      Cl  CH(OCH.sub.3).sub.2                             CH.sub.2 OCH.sub.3                                                                         H       H      Cl  CH(OCH.sub.3).sub.2                             OSO.sub.2 CHCl.sub.2                                                                       H       H      Cl  CH(OCH.sub.3).sub.2                             SC.sub.2 H.sub.5                                                                           H       H      Cl  CH(OCH.sub.3).sub.2                             OSO.sub.2 CH.sub.3                                                                         H       H      Cl  CH(OCH.sub.3).sub.2                             OSO.sub.2 C.sub.2 H.sub.5                                                                  H       H      Cl  CH(OCH.sub.3).sub.2                             CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                       H       H      Cl  CH(OCH.sub.3).sub.2                             SO.sub.2 C.sub.2 H.sub.5                                                                   H       H      Cl  CH(OCH.sub.3).sub.2                             NO.sub.2    5-CF.sub.3                                                                             H      Cl  CH(OCH.sub.3).sub.2                             SO.sub.2 -n-C.sub.3 H.sub.7                                                                3-Cl    H      Cl  CH(OCH.sub.3).sub.2                             OC.sub.2 H.sub.5                                                                           5-NO.sub.2                                                                             H      Cl  CH(OCH.sub.3).sub.2                             I           H       H      Cl  CH(OCH.sub.3).sub.2                             CO.sub.2 CH.sub.3                                                                          H       H      Cl  C(CH.sub.3)(OCH.sub.3).sub.2                    SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        6-NO.sub.2                                                                             H      Cl  CH(OCH.sub.3).sub.2                             Cl          5-Cl    H      Cl  CH(OCH.sub.3).sub.2                             SO.sub.2 CH.sub.3                                                                          5-Cl    H      Cl  CH(OCH.sub.3).sub.2                             CO.sub.2 CH.sub.3                                                                          4-F     H      Cl  CH(OCH.sub.3).sub.2                             ______________________________________                                    

                                      TABLE 1j                                     __________________________________________________________________________      ##STR44##                                                                     R.sub.7   R.sub.8                                                                             R.sub.21                                                                          X    Y        m.p.(°C.)                               __________________________________________________________________________     Cl        H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.3                                                                        H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     113-121°                                SO.sub.2 CH.sub.3                                                                        H    H  CH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     NO.sub.2  H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH(CH.sub.3).sub.2                                                              H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 C.sub.2 H.sub.5                                                                 H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CF.sub.3  H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Br        H    H  CH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     CH(CH.sub.3).sub.2                                                                       H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     C.sub.2 H.sub.5                                                                          H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2  -n-C.sub.3 H.sub.7                                                             H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 N(CH.sub.3).sub.2                                                               H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OCH.sub.2 CHCHCH.sub.3                                                                   H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OCF.sub.2 CF.sub.2 H                                                                     H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH.sub.2 OCH.sub.3                                                                       H    H  CH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     OSO.sub.2 CHCl.sub.2                                                                     H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SC.sub.2 H.sub.5                                                                         H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OSO.sub.2 CH.sub.3                                                                       H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OSO.sub.2 C.sub.2 H.sub.5                                                                H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                     H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 C.sub.2 H.sub.5                                                                 H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     NO.sub. 2 5-CF.sub.3                                                                          H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2  -n-C.sub.3 H.sub.7                                                             3-Cl H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OC.sub.2 H.sub.5                                                                         5-NO.sub.2                                                                          H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CH.sub.3                                                               H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     I         H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                      6-NO.sub.2                                                                          H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Cl        5-Cl H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                        5-Cl H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.3                                                                        4-F  H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OCH.sub.2 CHCH.sub.2                                                                     H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH(OCH.sub.3)CH.sub.3                                                                    H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 CF.sub.3                                                                        H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SCHF.sub.2                                                                               H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OCH.sub.2 CHCHCH.sub.3                                                                   H    H  CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Cl        H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.3                                                                        H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CH.sub.3                                                               H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                        H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 N(CH.sub.3).sub.2                                                               H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH(CH.sub.3).sub.2                                                                       H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OCH.sub.3 H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SCH.sub.3 H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2  -n-C.sub.3 H.sub.7                                                             H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      -n-C.sub.4 H.sub.9                                                                      H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     O -n-C.sub.4 H.sub.9                                                                     H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     NO.sub.2  H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2  -n-C.sub.4 H.sub.9                                                             H    CH.sub.3                                                                          CH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Cl        H    H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            CH.sub.2 OCH.sub.3                                                                       H    H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            SO.sub.2 C.sub.2 H.sub.5                                                                 H    H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            OCH.sub.3 H    H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            SC.sub.2 H.sub.5                                                                         H    H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            CO.sub.2 C.sub.2 H.sub.5                                                                 H    H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            CO.sub.2 CH.sub.3                                                                        5-Cl H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            Cl        H    H  CH.sub.3                                                                            CH(SCH.sub.3).sub.2                                     CO.sub.2 CH.sub.3                                                                        H    H  CH.sub.3                                                                            CH(SCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                        H    H  CH.sub.3                                                                            CH(SCH.sub.3).sub.2                                     NO.sub.2  H    H  CH.sub.3                                                                            CH(SCH.sub.3).sub.2                                     __________________________________________________________________________

                  TABLE 1k                                                         ______________________________________                                          ##STR45##                                                                     R.sub.7     R.sub.8                                                                              R.sub.21                                                                              X      Y       m.p.(°C.)                       ______________________________________                                         NO.sub.2    H     H      CH.sub.3                                                                              CH.sub.2 OTHP                                  Br          H     H      CH.sub.3                                                                              CH.sub.2 OTHP                                  Cl          H     H      CH.sub.3                                                                              CH.sub.2 OTHP                                  F           H     H      CH.sub.3                                                                              CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                          H     CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.2 OTHP                                  H           H     H      CH.sub.3                                                                              CH.sub.2 OTHP                                  CO.sub.2 CH.sub.3                                                                          H     H      CH.sub.3                                                                              CH.sub.2 OTHP                                  CH.sub.3    H     H      CH.sub.3                                                                              CH.sub.2 OTHP                                  SO.sub.2 N(CH.sub.3).sub.2                                                                 H     H      CH.sub.3                                                                              CH.sub.2 OTHP                                  SO.sub.2  -n-C.sub.3 H.sub.7                                                               H     H      CH.sub.3                                                                              CH.sub.2 OTHP                                  OCH.sub.3   H     H      CH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                  O -n-C.sub.3 H.sub.7                                                                       H     H      CH.sub.3                                                                              CH.sub.2 OTHP                                  CH.sub.2 OCH.sub.3                                                                         H     H      CH.sub.3                                                                              CH.sub.2 OTHP                                  CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H     H      CH.sub.3                                                                              CH.sub.2 OTHP                                  ______________________________________                                    

                  TABLE 1l                                                         ______________________________________                                          ##STR46##                                                                     R.sub.7     R.sub.8 R.sub.21                                                                              X      Ym.p.(°C.)                            ______________________________________                                         Cl          H       H      CH.sub.3                                                                              CH.sub.2 OH                                  CO.sub.2 CH.sub.3                                                                          H       CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.2 OH                                  SO.sub.2 CH.sub.3                                                                          H       H      CH.sub.3                                                                              CH.sub.2 OH                                  NO.sub.2    H       H      CH.sub.3                                                                              CH.sub.2 OH                                  CO.sub.2 CH(CH.sub.3).sub.2                                                                H       H      CH.sub.3                                                                              CH.sub.2 OH                                  CO.sub.2 C.sub.2 H.sub.5                                                                   H       H      CH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                  CF.sub.3    H       H      CH.sub.3                                                                              CH.sub.2 OH                                  Br          H       H      CH.sub.3                                                                              CH.sub.2 OH                                  CH.sub.3    H       H      CH.sub.3                                                                              CH.sub.2 OH                                  C.sub.2 H.sub.5                                                                            H       H      CH.sub.3                                                                              CH.sub. 2 OH                                 SO.sub.2  -n-C.sub.3 H.sub.7                                                               H       H      CH.sub.3                                                                              CH.sub.2 OH                                  SO.sub.2 N(CH.sub.3).sub.2                                                                 H       H      CH.sub.3                                                                              CH.sub.2 OH                                  OCH.sub.3   H       H      CH.sub.3                                                                              CH.sub.2 OH                                  CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H       CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.2 OH                                  OCF.sub.2 CF.sub.2 H                                                                       H       H      CH.sub.3                                                                              CH.sub.2 OH                                  CH.sub.2 OCH.sub.3                                                                         H       H      CH.sub.3                                                                              CH.sub.2 OH                                  OSO.sub.2 CHCl.sub.2                                                                       H       H      CH.sub.3                                                                              CH.sub.2 OH                                  SC.sub.2 H.sub.5                                                                           H       H      CH.sub.3                                                                              CH.sub.2 OH                                  OSO.sub.2 CH.sub.3                                                                         H       H      CH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                  OSO.sub.2 C.sub.2 H.sub.5                                                                  H       H      CH.sub.3                                                                              CH.sub.2 OH                                  CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                       H       H      CH.sub.3                                                                              CH.sub.2 OH                                  SO.sub.2 C.sub.2 H.sub.5                                                                   H       H      CH.sub.3                                                                              CH.sub.2 OH                                  NO.sub.2    5-CF.sub.3                                                                             H      CH.sub.3                                                                              CH.sub.2 OH                                  SO.sub.2  -n-C.sub.3 H.sub.7                                                               3-Cl    H      CH.sub.3                                                                              CH.sub.2 OH                                  OC.sub. 2 H.sub.5                                                                          5-NO.sub.2                                                                             H      CH.sub.3                                                                              CH.sub.2 OH                                  SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        6-NO.sub.2                                                                             H      CH.sub.3                                                                              CH.sub.2 OH                                  Cl          5-Cl    H      CH.sub.3                                                                              CH.sub.2 OH                                  SO.sub.2 CH.sub.3                                                                          5-Cl    H      CH.sub.3                                                                              CH.sub.2 OH                                  CO.sub.2 CH.sub.3                                                                          4-F     H      CH.sub.3                                                                              CH.sub.2 OH                                  ______________________________________                                    

                                      TABLE 1m                                     __________________________________________________________________________      ##STR47##                                                                     R.sub.7   R.sub.8                                                                            R.sub.21                                                                          X    Y            m.p.(°C.)                            __________________________________________________________________________     NO.sub.2  H   H  CH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                               NO.sub.2  H   CH.sub.3                                                                          CH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                     NO.sub.2  H   H  CH.sub.3                                                                            CH.sub.2 SCH.sub.3                                       Br        H   H  CH.sub.3                                                                            CH.sub.2 OCONHCH.sub.3                                   Cl        H   H  CH.sub.3                                                                            CH.sub.2 OCO.sub.2 CH.sub.3                              F         H   H  CH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                                F         H   H  CH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                 SO.sub.2 CH.sub.3                                                                        H   H  CH.sub.2 CH.sub.3                                                                   CH.sub.2 OCOC.sub.2 H.sub.5                              SO.sub.2 CH.sub.3                                                                        H   H  CH.sub.3                                                                            CH(OCH(CH.sub.3)CH.sub.2 O)                              SO.sub.2 CH.sub.3                                                                        H   H  CH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                        SO.sub.2 CH.sub.3                                                                        H   H  CH.sub.3                                                                            CH.sub.2 SCH.sub.2 CH.sub.3                              H         H   H  CH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                     CO.sub.2 CH.sub.3                                                                        H   H  CH.sub.3                                                                            CH.sub.2 OCON(CH.sub.3).sub.2                            CO.sub.2 CH.sub.3                                                                        H   H  CH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                 CO.sub.2 CH.sub.3                                                                        H   CH.sub.3                                                                          CH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                     CO.sub.2 CH.sub.3                                                                        H   H  CH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                                CH.sub.3  H   H  CH.sub.2 CH.sub.3                                                                   CH(OC.sub.2 H.sub.5).sub.2                               CH.sub.3  H   H  CH.sub.3                                                                            CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                       SO.sub.2 N(CH.sub.3).sub.2                                                               H   H  CH.sub.3                                                                            CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                     SO.sub.2 N(CH.sub.3).sub.2                                                               H   H  CH.sub.3                                                                            CH.sub.2 OCO -i-C.sub.3 H.sub.7                          SO.sub.2  -n-C.sub.3 H.sub.7                                                             H   H  CH.sub.3                                                                            CH.sub.2 OCONH -n-C.sub.3 H.sub.7                        SO.sub. 2 H-n-C.sub.3 H.sub.7                                                                H  CH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                               OCH.sub.3 H   H  CH.sub.3                                                                            CH(SCH.sub.2 CH.sub.2 S)                                 OCH.sub.3 H   H  CH.sub.3                                                                            CH.sub.2 SCH.sub.3                                       O -n-C.sub.3 H.sub.7                                                                     H   H  CH.sub.3                                                                            CH.sub.2 OCO.sub.2 CH.sub.3                              Cl        H   H  CH.sub.3                                                                            C(CH.sub.3)(SCH.sub.3).sub.2                             CO.sub.2 CH.sub.3                                                                        H   H  CH.sub.3                                                                            CH(C.sub.2 H.sub.5)SCH.sub.3                             SO.sub.2 N(CH.sub.3).sub.2                                                               H   H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                        I         H   H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.2 CH.sub.2 CH.sub.2 O)               Br        H   CH.sub.3                                                                          OCH.sub.3                                                                           CH.sub.2 OCONHCH.sub.3                                   CF.sub.3  H   H  OCH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                 CF.sub.3  H   H  OCH.sub.3                                                                           CH.sub.2 SEt                                             SO.sub.2 N(Et).sub.2                                                                     H   H  OCH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                 OCH.sub.2 CH.sub.3                                                                       H   H  OC.sub.2 H.sub.5                                                                    CH(OCH.sub.2 CH.sub.2 O)                                 O -n-C.sub.4 H.sub.9                                                                     H   H  OCH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                 O- -i-C.sub.3 H.sub.7                                                                    H   H  OCH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                 OCH.sub.2 CHCH.sub.2                                                                     H   H  OCH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                 SO.sub.2 CF.sub.3                                                                        H   H  OCH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                 SO.sub.2 CF.sub.3                                                                        5-CF.sub.3                                                                         H  OCH.sub.3                                                                           CH(OEt).sub.2                                            SO.sub.2 CF.sub.3                                                                        H   H  OCH.sub.3                                                                           CH(OEt).sub.2                                            SO.sub.2  -n-C.sub.3 H.sub.7                                                             H   H  OCH.sub.3                                                                           CH(OEt).sub.2                                            SO.sub.2  -n-C.sub.3 H.sub.7                                                             H   CH.sub.3                                                                          OCH.sub.3                                                                           CH(OEt).sub.2                                            SO.sub.2  -n-C.sub.3 H.sub.7                                                             H   H  OCH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                 OCF.sub.2 CF.sub.2 H                                                                     H   H  OCH.sub.3                                                                           CH.sub.2 OCOCH.sub.3                                     OCF.sub.2 CF.sub.2 H                                                                     H   H  OC.sub.2 H.sub.5                                                                    CH.sub.2 OCOCH.sub.3                                     OCF.sub.2 CF.sub.2 H                                                                     H   H  OCH.sub.3                                                                           CH.sub.2 OCOCH.sub.3                                     OSO.sub.2 C.sub.2 H.sub.5                                                                H   H  OCH.sub.3                                                                           CH.sub.2 OCOCH.sub.3                                     CH.sub.2 OEt                                                                             6-F H  OCH.sub.3                                                                           CH.sub. 2 OCOCH.sub.3                                    CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                            H   H  OCH.sub.3                                                                           CH(OCH(CH.sub.3)CH.sub.2 O)                              SO.sub.2 N(CH.sub.3)Et                                                                   H   H  OCH.sub.3                                                                           CH.sub.2 OCO.sub.2 Et                                    SO.sub.2 N(CH.sub.3)Et                                                                   H   H  OCH.sub.3                                                                           CH.sub.2 OCON(CH.sub.3).sub.2                            SO.sub.2 N(CH.sub.3)Et                                                                   H   H  OCH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                        Cl        H   H  OCH.sub.3                                                                           CH.sub.2 SCH.sub.3                                       CO.sub.2 CH.sub.3                                                                        H   H  OCH.sub.3                                                                           CH.sub.2 SCH.sub.3                                       CO.sub.2 CH.sub.2 CH.sub.3                                                               H   H  OCH.sub.3                                                                           CH.sub.2 SCH.sub.3                                       SO.sub.2 N(CH.sub.3).sub.2                                                               H   H  OCH.sub.3                                                                           CH.sub.2 SCH.sub.3                                       NO.sub.2  H   H  OCH.sub.3                                                                           CH.sub.2 SCH.sub.3                                       SO.sub.2 CH.sub.3                                                                        H   H  OCH.sub.3                                                                           CH.sub.2 SCH.sub.3                                       Cl        H   H  OCH.sub.3                                                                           CH.sub.2 SO.sub.2 CH.sub.3                               CO.sub.2 CH.sub.3                                                                        H   H  OCH.sub.3                                                                           CH.sub.2 SO.sub.2 CH.sub.3                               O -n-C.sub.3 H.sub.7                                                                     H   H  CH.sub.3                                                                            CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                     CH.sub.2 OCH.sub.3                                                                       H   H  CH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                     CH.sub.2 OCH.sub.3                                                                       H   H  CH.sub.3                                                                            CH.sub.2 OCO.sub.2 CH.sub.3                              CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H   H  CH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                               SO.sub.2 CH.sub.3                                                                        H   H  CH.sub.3                                                                            CH.sub.2 S(O)CH.sub.3                                    Cl        H   H  CH.sub.3                                                                            CH.sub.2 S(O)CH.sub.3                                    CO.sub.2 CH.sub.3                                                                        H   H  CH.sub.3                                                                            CH.sub.2 S(O)CH.sub.3                                    OCH.sub.3 H   H  OCH.sub.3                                                                           CH(CH.sub.3)(S(O)CH.sub.3)                               CH.sub.2 OCH.sub.3                                                                       H   H  OCH.sub.3                                                                           CH(CH.sub.3)(S(O)CH.sub.3)                               __________________________________________________________________________

                                      TABLE 1n                                     __________________________________________________________________________      ##STR48##                                                                     R.sub.7   R.sub.8                                                                            R.sub.21                                                                          X     Y        m.p.(°C.)                               __________________________________________________________________________     Cl        H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     117-121°                                CO.sub.2 CH.sub.3                                                                        H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                                                     135-158°                                SO.sub.2 CH.sub.3                                                                        H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     NO.sub.2  H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH(CH.sub.3).sub.2                                                              H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 C.sub.2 H.sub.5                                                                 H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CF.sub.3  H   H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     Br        H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH.sub.3  H   H  OCH.sub.3                                                                            CH(OCH.sub. 3).sub.2                                    C.sub.2 H.sub.5                                                                          H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2  -n-C.sub.3 H.sub.7                                                             H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 N(CH.sub.3).sub.2                                                               H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OCH.sub.3 H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H   CH.sub.3                                                                          OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     OCF.sub.2 CF.sub.2 H                                                                     H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH.sub.2 OCH.sub.3                                                                       H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OSO.sub.2 CHCl.sub.2                                                                     H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SC.sub.2 H.sub.5                                                                         H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OSO.sub.2 CH.sub.3                                                                       H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     OSO.sub.2 C.sub.2 H.sub.5                                                                H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                     H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 C.sub.2 H.sub.5                                                                 H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     NO.sub.2  5-CF.sub.3                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2  -n-C.sub.3 H.sub.7                                                             3-Cl                                                                               H  OCH.sup.3                                                                            CH(OCH.sub.3).sub.2                                     OC.sub.2 H.sub.5                                                                         5-NO.sub.2                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH.sub.2 CH.sub.3                                                                        H   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            CO.sub.2 CH.sub.3                                                                        H   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            CH.sub.2 Cl                                                                              H   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                      6-NO.sub.2                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Cl        5-Cl                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                        5-Cl                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.3                                                                        4-F H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH.sub.2 CH.sub.3                                                               H   H  OCH.sub.3                                                                            C(C.sub.2 H.sub.5)(OCH.sub.3).sub.2                     I         H   H  OCH.sub.3                                                                            C(C.sub.2 H.sub.5)(OCH.sub.3).sub.2                     Cl        H   H  OCH.sub.3                                                                            C(C.sub.2 H.sub.5)(OCH.sub.3).sub.2                     __________________________________________________________________________

                  TABLE 1o                                                         ______________________________________                                          ##STR49##                                                                                                               m.p.                                 R.sub.7     R.sub.8                                                                               R.sub.21                                                                              X       Y       (°C.)                         ______________________________________                                         NO.sub.2    H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                Br          H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                Cl          H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                                                          136-                                                                           139°                          SO.sub.2 CH.sub.3                                                                          H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                F           H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                H           H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                CO.sub.2 CH.sub.3                                                                          H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                CH.sub.3    H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                SO.sub.2 N(CH.sub.3).sub.2                                                                 H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                SO.sub.2  -n-C.sub.3 H.sub.7                                                               H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                OCH.sub.3   H      CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OTHP                                O -n-C.sub.3 H.sub.7                                                                       H      H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                CH.sub.2 OCH.sub.3                                                                         H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                I           H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                CH.sub.2 Cl H      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                ______________________________________                                    

                  TABLE 1p                                                         ______________________________________                                          ##STR50##                                                                                                               m.p.                                 R.sub.7     R.sub.8 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         Cl          H       H      OCH.sub.3                                                                              CH.sub.2 OH                                                                           133-                                                                           135°                          CO.sub.2 CH.sub.3                                                                          H       H      OCH.sub.3                                                                              CH.sub.2 OH                                                                           115°                                                                    d                                    SO.sub.2 CH.sub.3                                                                          H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 NO.sub.2    H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                                H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 C.sub.2 H.sub.5                                                                   H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CF.sub.3    H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 Br          H       H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 CH.sub.3    H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 C.sub.2 H.sub.5                                                                            H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                                H       H      OCH.sub.3                                                                              CH.sub.2 OH                                                                           152°                                                                    d                                    SO.sub.2 N(CH.sub.3).sub.2                                                                 H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 OCH.sub.3   H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 OCF.sub.2 CF.sub.2 H                                                                       H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CH.sub.2 OCH.sub.3                                                                         H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 OSO.sub.2 CHCl.sub.2                                                                       H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 SC.sub.2 H.sub.5                                                                           H       CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                                 OSO.sub.2 CH.sub.3                                                                         H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 OSO.sub.2 C.sub.2 H.sub.5                                                                  H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                       H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 C.sub.2 H.sub.5                                                                   H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 NO.sub.2    5-CF.sub.3                                                                             H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 SO.sub.2 - n-C.sub.3 H.sub.7                                                               3-Cl    H      OCH.sub.3                                                                              CH.sub.2 OH                                 OC.sub.2 H.sub.5                                                                           5-NO.sub.2                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 I           H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 CH.sub.2 Cl H       H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                        6-NO.sub.2                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 Cl          5-Cl    H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                          5-Cl    H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH.sub.3                                                                          4-F     H      OCH.sub.3                                                                              CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 1q                                     __________________________________________________________________________      ##STR51##                                                                     R.sub.7   R.sub.8                                                                          R.sub.21                                                                          X     Y           m.p.(°C.)                              __________________________________________________________________________     NO.sub.2  H H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5)2                                     NO.sub.2  H H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                      NO.sub.2  H H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                        Br        H H  OCH.sub.3                                                                            CH.sub.2 OCONHCH.sub.3                                    Cl        H H  OCH.sub.3                                                                            CH.sub.2 OCO.sub.2 CH.sub.3                               F         H H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                                 F         H H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                  SO.sub.2 CH.sub.3                                                                        H H  OCH.sub.3                                                                            CH.sub.2 OCOC.sub.2 H.sub.5                               SO.sub.2 CH.sub.3                                                                        H H  OCH.sub.3                                                                            CH(OCH(CH.sub.3)CH.sub.2 O)                               SO.sub.2 CH.sub.3                                                                        H H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                         SO.sub.2 CH.sub.3                                                                        H H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 SCH.sub.3                                        H         H H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                      CO.sub.2 CH.sub.3                                                                        H H  OCH.sub.3                                                                            CH.sub.2 OCON(CH.sub.3).sub.2                             CO.sub.2 CH.sub.3                                                                        H H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                  CO.sub.2 CH.sub.3                                                                        H H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                      CO.sub.2 CH.sub.3                                                                        H CH.sub.3                                                                          OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                                 CH.sub.3  H H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                CH.sub.3  H H  OCH.sub.3                                                                            CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                        SO.sub.2 N(CH.sub.3).sub.2                                                               H H  OCH.sub.3                                                                            CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                      SO.sub.2 N(CH.sub.3).sub.2                                                               H H  OCH.sub.3                                                                            CH.sub.2 OCO -i-C.sub.3 H.sub.7                           SO.sub.2 -n-C.sub.3 H.sub.7                                                              H H  OCH.sub.3                                                                            CH.sub.2 OCONH -n-C.sub.3 H.sub.7                         SO.sub.2 -n-C.sub.3 H.sub.7                                                              H H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                OCH.sub.3 H H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.2 CH.sub.2 O)                                  OCH.sub.3 H H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                        O -n-C.sub.3 H.sub.7                                                                     H H  OCH.sub.3                                                                            CH.sub.2 OCO.sub.2 CH.sub.3                               NO.sub.2  H H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                                SO.sub.2 CH.sub.3                                                                        H H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                                CO.sub.2 CH.sub.3                                                                        H H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                                CO.sub.2 CH.sub.2 CH.sub.3                                                               H H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                                O -n-C.sub.3 H.sub.7                                                                     H H  OCH.sub.3                                                                            CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                      CH.sub.2 OCH.sub.3                                                                       H H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                      CH.sub.2 OCH.sub.3                                                                       H H  OCH.sub.3                                                                            CH.sub.2 OCO.sub.2 CH.sub.3                               CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                I         H H  OCH.sub.3                                                                            CH(CH.sub.3)SCH.sub.3                                     CH.sub.2 Cl                                                                              H H  OCH.sub.3                                                                            CH(C.sub.2 H.sub.5)SO.sub.2 CH.sub.3                      CO.sub.2 CH.sub.2 CH.sub.3                                                               H H  OCH.sub.3                                                                            C(CH.sub.3)(SCH.sub.2 CH.sub.2 S)                         NO.sub.2  H H  OCH.sub.3                                                                            C(C.sub.2 H.sub.5)(SCH.sub.3).sub.2                       SO.sub.2 N(CH.sub.3).sub.2                                                               H H  OCH.sub.3                                                                            CH(SC.sub.2 H.sub.5).sub.2                                OCHF.sub.2                                                                               H H  OCH.sub.3                                                                            CH(SCH.sub.3).sub.2                                       Cl        H H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                       Br        H H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                                CH.sub.2 OCH.sub.3                                                                       H H  OCH.sub.3                                                                            C(CH.sub.3)(SCH.sub.3).sub.2                              SO.sub.2 N(CH.sub.3).sub.2                                                               H H  OCH.sub.3                                                                            CH.sub.2 S(O)CH.sub.3                                     NO.sub.2  H H  OCH.sub.3                                                                            CH.sub.2 S(O)CH.sub.2 CH.sub.3                            CH.sub.2 OCH.sub.3                                                                       H H  OCH.sub.3                                                                            CH.sub.2 S(O)CH.sub.3                                     SO.sub.2 CH.sub.3                                                                        H H  OCH.sub.3                                                                            CH(CH.sub.3)(S(O)CH.sub.3)                                CO.sub.2 CH.sub.3                                                                        H H  OCH.sub.3                                                                            CH(CH.sub.3)(S(O)CH.sub.3)                                __________________________________________________________________________

                  TABLE 1r                                                         ______________________________________                                          ##STR52##                                                                                                           m.p.                                     R.sub.7  R.sub.8 X       Y            Z(°C.)                            ______________________________________                                         H        H       CH.sub.3                                                                               CH(OCH.sub.3).sub.2                                                                         CH                                       H        H       OCH.sub.3                                                                              CH.sub.2 SCH.sub.3                                                                          CH                                       Cl       H       CH.sub.3                                                                               CH.sub.2 SO.sub.2 CH.sub.3                                                                  CH                                       Cl       H       OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                                                           CH                                       Cl       H       CH.sub.3                                                                               CH(OCH.sub.3).sub.2                                                                         CH                                       Cl       5-Cl    OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                                                                         N                                        NO.sub.2 H       CH.sub.3                                                                               CH(OCH.sub.3).sub.2                                                                         N                                        NO.sub.2 H       OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                                                                         CH                                       CO.sub.2 CH.sub.3                                                                       H       CH.sub.3                                                                               CH(OCH.sub.3).sub.2                                                                         CH                                       CO.sub.2 CH.sub.3                                                                       H       OCH.sub.3                                                                              CH(OEt).sub.2                                                                               CH                                       CO.sub.2 CH.sub.3                                                                       H       OC.sub.2 H.sub.5                                                                       CH(OEt).sub.2                                                                               CH                                       CO.sub.2 CH.sub.2 CH.sub.3                                                              H       CH.sub.3                                                                               CH.sub.2 OTHP                                                                               N                                        CO.sub.2 CH.sub.2 CH.sub.3                                                              H       C.sub.2 H.sub.5                                                                        CH.sub.2 OH  N                                        CO.sub.2 CH.sub.2 CH.sub.3                                                              H       Cl      CH.sub.2 SCH.sub.3                                                                          N                                        SO.sub.2 CH.sub.3                                                                       H       CH.sub.3                                                                               CH(CH.sub.3)SC.sub.2 H.sub.5                                                                CH                                       SO.sub.2 CH.sub.3                                                                       H       OC.sub.2 H.sub.5                                                                       CH(CH.sub.3)SC.sub.2 H.sub.5                                                                CH                                       SO.sub.2 CH.sub.3                                                                       H       CH.sub.3                                                                               CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                           CH                                       SC.sub.2 H.sub.5                                                                        H       OCH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                           N                                        SC.sub.2 H.sub.5                                                                        H       CH.sub.3                                                                               CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                           N                                        SC.sub.2 H.sub.5                                                                        H       OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                                                                         CH                                       SO.sub.2 N(CH.sub.3).sub.2                                                              H       C.sub.2 H.sub.5                                                                        CH(OCH.sub.3).sub.2                                                                         CH                                       SO.sub.2 N(CH.sub.3).sub.2                                                              3-CH.sub.3                                                                             OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                                                                         CH                                       SO.sub.2 N(CH.sub.3).sub.2                                                              H       CH.sub.3                                                                               CH(OCH.sub.3).sub.2                                                                         CH                                       C.sub.2 H.sub.5                                                                         H       OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                                                                         CH                                       C.sub.2 H.sub.5                                                                         H       CH.sub.3                                                                               CH(CH.sub.3)SO.sub.2 CH.sub.3                                                               N                                        C.sub.2 H.sub.5                                                                         H       OCH.sub.3                                                                              CH(CH.sub.3)SO.sub.2 CH.sub.3                                                               N                                        C.sub.2 H.sub.5                                                                         H       OCH.sub.3                                                                              CH(CH.sub.3)SO.sub.2 CH.sub.3                                                               CH                                       O -i-C.sub.3 H.sub.7                                                                    H       CH.sub.3                                                                               CH(OCH.sub.2 CH.sub.2 O)                                                                    CH                                       O -i-C.sub.3 H.sub.7                                                                    H       OCH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                                                                    CH                                       F        H       CH.sub.3                                                                               CH(OCH.sub.2 CH.sub.2 O)                                                                    CH                                       Br       H       OCH.sub.3                                                                              CH(OCH(CH.sub.3)CH.sub.2 O)                                                                 N                                        CH.sub.2 OCH.sub.3                                                                      H       CH.sub.3                                                                               CH(SCH.sub.2 CH.sub.2 S)                                                                    CH                                       CH.sub.2 OCH.sub.3                                                                      H       OCH.sub.3                                                                              CH(SCH.sub.3).sub.2                                                                         CH                                       CH.sub.2 OCH.sub.3                                                                      6-Cl    OCH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                                                                  CH                                       SO.sub.2 -n-C.sub.3 H.sub.7                                                             H       CH.sub.3                                                                               CH(CH.sub.3)SCH.sub.3                                                                       CH                                       CO.sub.2 CH.sub.3                                                                       H       OCH.sub.3                                                                              CH.sub.2 S(O)CH.sub.3                                                                       CH                                       CO.sub.2 CH.sub.3                                                                       H       OCH.sub.3                                                                              CH.sub.2 S(O)CH.sub.3                                                                       N                                        ______________________________________                                    

                  TABLE 2a                                                         ______________________________________                                          ##STR53##                                                                                                               m.p.                                 R.sub.14 R.sub.15 R.sub.21                                                                              X       Y        (°C.)                         ______________________________________                                         Cl       H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           Br       H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           F        H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           H        H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           Cl       H        H      Cl      CH(OCH.sub.3).sub.2                           Cl       3-Cl     H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           Cl       H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           OCH.sub.3                                                                               H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           CH.sub.3 H        H      OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                           Br       H        H      Cl      CH(OCH.sub.3).sub.2                           CH.sub.3 H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           NO.sub.2 H        CH.sub.3                                                                              OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           CH.sub.3 4-F      H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           Cl       6-NO.sub.2                                                                              H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           NO.sub.2 H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           NO.sub.2 H        H      Cl      CH(OCH.sub.3).sub.2                           Cl       6-F      H      CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.3).sub.2                           NO.sub.2 4-Cl     H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           Cl       5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           F        H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           H        H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                           SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                           OCH.sub.3                                                                               H        CH.sub.3                                                                              CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           OSO.sub.2 CH.sub.3                                                                      H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                           Cl       H        H      CH.sub.3                                                                               C(CH.sub.3)(OCH.sub.3).sub.2                  Br       H        H      CH.sub.3                                                                               C(C.sub.2 H.sub.5)(OCH.sub.3).sub.2           OCH.sub.3                                                                               H        H      CH.sub.3                                                                               C(CH.sub.3)(OCH.sub.3).sub.2                  NO.sub.2 H        H      CH.sub.3                                                                               C(CH.sub.3)(OCH.sub.3).sub.2                  ______________________________________                                    

                  TABLE 2b                                                         ______________________________________                                          ##STR54##                                                                                                               m.p.                                 R.sub.14 R.sub.15 R.sub.21                                                                               X       Y       (°C.)                         ______________________________________                                         Cl       H        H       CH.sub.3                                                                               CH.sub.2 OTHP                                Br       H        H       CH.sub.3                                                                               CH.sub.2 OTHP                                F        H        H       OCH.sub.3                                                                              CH.sub.2 OTHP                                H        H        H       OCH.sub.3                                                                              CH.sub.2 OTHP                                Cl       3-Cl     H       CH.sub.3                                                                               CH.sub.2 OTHP                                Cl       H        H       OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                OCH.sub.3                                                                               H        H       CH.sub.3                                                                               CH.sub.2 OTHP                                CH.sub.3 H        CH.sub.3                                                                               OCH.sub.3                                                                              CH.sub.2 OTHP                                CH.sub.3 H        H       CH.sub.3                                                                               CH.sub.2 OTHP                                NO.sub.2 H        H       OCH.sub.3                                                                              CH.sub.2 OTHP                                CH.sub.3 4-F      H       OCH.sub.3                                                                              CH.sub.2 OTHP                                Cl       6-NO.sub.2                                                                              H       OCH.sub.3                                                                              CH.sub.2 OTHP                                NO.sub.2 H        H       CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                                Cl       6-F      H       CH.sub.3                                                                               CH.sub.2 OTHP                                NO.sub.2 4-Cl     H       CH.sub.3                                                                               CH.sub.2 OTHP                                Cl       5-OCH.sub.3                                                                             H       OCH.sub.3                                                                              CH.sub.2 OTHP                                F        H        H       CH.sub.3                                                                               CH.sub.2 OTHP                                H        H        H       CH.sub.3                                                                               CH.sub.2 OTHP                                SO.sub.2 N(CH.sub.3).sub.2                                                              H        H       OCH.sub.3                                                                              CH.sub.2 OTHP                                SO.sub.2 N(CH.sub.3).sub.2                                                              H        H       OCH.sub.3                                                                              CH.sub.2 OTHP                                OCH.sub.3                                                                               H        H       CH.sub.3                                                                               CH.sub.2 OTHP                                OSO.sub.2 CH.sub.3                                                                      H        H       CH.sub.3                                                                               CH.sub.2 OTHP                                ______________________________________                                    

                  TABLE 2c                                                         ______________________________________                                          ##STR55##                                                                                                               m.p.                                 R.sub.14  R.sub.15 R.sub.21                                                                              X        Y      (°C.)                         ______________________________________                                         Cl        H        H      CH.sub.3 CH.sub.2 OH                                 Br        H        H      CH.sub.3 CH.sub.2 OH                                 F         H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 H         H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 Cl        3-Cl     H      CH.sub.3 CH.sub.2 OH                                 Cl        H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 OCH.sub.3 H        H      CH.sub.2 CH.sub.3                                                                       CH.sub.2 OH                                 CH.sub.3  H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 CH.sub.3  H        H      CH.sub.3 CH.sub.2 OH                                 NO.sub.2  H        CH.sub.3                                                                              OCH.sub.3                                                                               CH.sub.2 OH                                 CH.sub.3  4-F      H      OCH.sub.3                                                                               CH.sub.2 OH                                 Cl        6-NO.sub.2                                                                              H      OCH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 NO.sub.2  H        H      CH.sub.3 CH.sub.2 OH                                 Cl        6-F      H      CH.sub.3 CH.sub.2 OH                                 NO.sub.2  4-Cl     H      CH.sub.3 CH.sub.2 OH                                 Cl        5-OCH.sub.3                                                                             H      OCH.sub.3                                                                               CH.sub.2 OH                                 F         H        H      CH.sub.3 CH.sub.2 OH                                 H         H        H      CH.sub.3 CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                               H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                               H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 OCH.sub.3 H        H      CH.sub.3 CH.sub.2 OH                                 OSO.sub.2 CH.sub.3                                                                       H        CH.sub.3                                                                              CH.sub.3 CH.sub.2 OH                                 SO.sub.2  -n-C.sub.3 H.sub.7                                                             H        H      OCH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 2d                                     __________________________________________________________________________      ##STR56##                                                                     R.sub.14                                                                              R.sub.15                                                                            R.sub.21                                                                          X    Y            m.p. (°C.)                             __________________________________________________________________________     Cl     H    H  CH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                   Br     H    H  CH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                       F      H    H  OCH.sub.3                                                                           CH.sub.2 SC.sub.2 H.sub.5                                  H      H    H  OCH.sub.3                                                                           CH.sub.2 OCO.sub.2 CH.sub.3                                Cl     3-Cl H  CH.sub.3                                                                            CH.sub.2 SCH.sub.3                                         Cl     H    H  OCH.sub.3                                                                           CH(OC.sub.2 H.sub.5).sub.2                                 OCH.sub.3                                                                             H    H  CH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                          CH.sub.3                                                                              H    H  OCH.sub.3                                                                           CH.sub.2 OCO .sub.-i-C.sub.3 H.sub.7                       CH.sub. 3                                                                             H    H  CH.sub.3                                                                            CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                         NO.sub.2                                                                              H    H  OCH.sub.3                                                                           CH(OC.sub.2 H.sub.5).sub.2                                 CH.sub.3                                                                              4-F  CH.sub.3                                                                          OCH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                   Cl     6-NO.sub.2                                                                          H  OCH.sub.3                                                                           CH.sub.2 OCOCH.sub.3                                       NO.sub.2                                                                              H    H  CH.sub.3                                                                            CH.sub.2 OCOC.sub.2 H.sub.5                                Cl     6-F  H  CH.sub.3                                                                            CH.sub.2 OCO.sub.2  -n-C.sub.3 H.sub.7                     NO.sub.2                                                                              4-Cl H  CH.sub.3                                                                            CH.sub.2 SCH.sub.3                                         Cl     5-OCH.sub.3                                                                         H  OCH.sub.3                                                                           CH.sub.2 SC.sub.2 H.sub.5                                  F      H    H  CH.sub.3                                                                            CH(SCH(CH.sub.3)CH.sub.2 S)                                H      H    H  CH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                 SO.sub.2 N(CH.sub.3).sub.2                                                            H    H  OCH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                   SO.sub.2 N(CH.sub.3).sub.2                                                            H    H  OCH.sub.3                                                                           CH.sub.2 OCONHCH.sub.3                                     OCH.sub.3                                                                             H    H  CH.sub.3                                                                            CH.sub.2 OCONH -n-C.sub.3 H.sub.7                          OSO.sub.2 CH.sub.3                                                                    H    H  CH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                       SO.sub.2  -n-C.sub. 3 H.sub.7                                                         H    H  OCH.sub.3                                                                           CH(OC.sub.2 H.sub.5).sub.2                                 Cl     H    H  OCH.sub.3                                                                           CH(SCH.sub.3).sub.2                                        NO.sub.2                                                                              H    H  OCH.sub.3                                                                           CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                        OSO.sub.2 CH.sub.3                                                                    H    H  OCH.sub.3                                                                           CH(CH.sub.3)SCH.sub.3                                      CH.sub.3                                                                              H    H  OCH.sub.3                                                                           CH.sub.2 SO.sub.2 CH.sub.3                                 SO.sub.2 CH.sub.3                                                                     H    H  OCH.sub.3                                                                           C(CH.sub.3)(SCH.sub.2 CH.sub.2 CH.sub.2 S)                 __________________________________________________________________________

                                      TABLE 2e                                     __________________________________________________________________________      ##STR57##                                                                     R.sub.14                                                                              R.sub.15                                                                            R.sub.21                                                                          X      Y          m.p. (°C.)                             __________________________________________________________________________     Cl     H    H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                      Br     H    H  CH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                                      F      H    H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H      H    H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      Cl     3-Cl H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                      Cl     H    H  OCH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                      OCH.sub.3                                                                             H    H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                      CH.sub.3                                                                              H    H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      CH.sub.3                                                                              H    CH.sub.3                                                                          CH.sub.3                                                                              CH(OCH.sub.3).sub. 2                                     NO.sub.2                                                                              H    H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      CH.sub.3                                                                              4-F  H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      Cl     6-NO.sub.2                                                                          H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      NO.sub.2                                                                              H    H  CH.sub.2                                                                              CH(OCH.sub.3).sub.2                                      Cl     6-F  H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                      NO.sub.2                                                                              4-Cl H  CH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                                      Cl     5-OCH.sub.3                                                                         H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      F      H    H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                      H      H    H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                      SO.sub.2 N(CH.sub.3).sub.2                                                            H    H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      SO.sub.2 N(CH.sub.3).sub.2                                                            H    H  OCH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                      OCH.sub.3                                                                             H    H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                      OSO.sub.2 CH.sub.3                                                                    H    H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                      SO.sub.2  -n-C.sub.3 H.sub.7                                                          H    H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      OCH.sub.3                                                                             H    H  OCH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                             Cl     H    H  OCH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                             F      H    H  OCH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                             SO.sub.2 CH.sub.2 CH.sub.3                                                            H    H  CH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                             NO.sub.2                                                                              H    H  OCH.sub.3                                                                             C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2                    __________________________________________________________________________

                  TABLE 2f                                                         ______________________________________                                          ##STR58##                                                                                                               m.p.                                 R.sub.14 R.sub.15 R.sub.21                                                                              X        Y       (°C.)                         ______________________________________                                         Cl       H        CH.sub.3                                                                              CH.sub.2 CH.sub.3                                                                       CH.sub.2 OTHP                                Br       H        H      CH.sub.3 CH.sub.2 OTHP                                F        H        H      OCH.sub.3                                                                               CH.sub.2 OTHP                                H        H        H      OCH.sub.3                                                                               CH.sub.2 OTHP                                Cl       3-Cl     H      CH.sub.3 CH.sub.2 OTHP                                Cl       H        H      OCH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                                OCH.sub.3                                                                               H        H      CH.sub.3 CH.sub.2 OTHP                                CH.sub.3 H        H      OCH.sub.3                                                                               CH.sub.2 OTHP                                CH.sub.3 H        H      CH.sub.3 CH.sub.2 OTHP                                NO.sub.2 H        H      OCH.sub.3                                                                               CH.sub.2 OTHP                                CH.sub.3 4-F      H      OCH.sub.3                                                                               CH.sub.2 OTHP                                Cl       6-NO.sub.2                                                                              H      OCH.sub.3                                                                               CH.sub.2 OTHP                                NO.sub.2 H        H      CH.sub.3 CH.sub.2 OTHP                                Cl       6-F      H      CH.sub.3 CH.sub.2 OTHP                                NO.sub.2 4-Cl     H      CH.sub.3 CH.sub.2 OTHP                                Cl       5-OCH.sub.3                                                                             H      OCH.sub.3                                                                               CH.sub.2 OTHP                                F        H        H      CH.sub.3 CH.sub.2 OTHP                                H        H        H      CH.sub.3 CH.sub.2 OTHP                                SO.sub.2 N(CH.sub.3).sub.2                                                              H        CH.sub.3                                                                              OCH.sub.3                                                                               CH.sub.2 OTHP                                SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                               CH.sub.2 OTHP                                OCH.sub.3                                                                               H        H      CH.sub.2 CH.sub.3                                                                       CH.sub.2 OTHP                                OSO.sub.2 CH.sub.3                                                                      H        H      CH.sub.3 CH.sub.2 OTHP                                SO.sub.2 H-n-C.sub.3 H.sub.7                                                                     H      OCH.sub.3                                                                               CH.sub.2 OTHP                                ______________________________________                                    

                  TABLE 2g                                                         ______________________________________                                          ##STR59##                                                                                                               m.p.                                 R.sub.14  R.sub.15 R.sub.21                                                                              X        Y      (°C.)                         ______________________________________                                         Cl        H        H      CH.sub.3 CH.sub.2 OH                                 Br        H        H      CH.sub.3 CH.sub.2 OH                                 F         H        H      OCH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 H         H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 Cl        3-Cl     H      CH.sub.3 CH.sub.2 OH                                 Cl        H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 OCH.sub.3 H        H      CH.sub.3 CH.sub.2 OH                                 CH.sub.3  H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 CH.sub.3  H        H      CH.sub.3 CH.sub.2 OH                                 NO.sub.2  H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 CH.sub.3  4-F      H      OCH.sub.3                                                                               CH.sub.2 OH                                 Cl        6-NO.sub.2                                                                              H      OCH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2  H        H      CH.sub.3 CH.sub.2 OH                                 Cl        6-F      H      CH.sub.3 CH.sub.2 OH                                 NO.sub.2  4-Cl     H      CH.sub.3 CH.sub.2 OH                                 Cl        5-OCH.sub.3                                                                             H      OCH.sub.3                                                                               CH.sub.2 OH                                 F         H        H      CH.sub.3 CH.sub.2 OH                                 H         H        H      CH.sub.3 CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                               H        CH.sub.3                                                                              OCH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                               H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 OCH.sub.3 H        H      CH.sub.3 CH.sub.2 OH                                 OSO.sub.2 CH.sub.3                                                                       H        H      CH.sub.2 CH.sub.3                                                                       CH.sub.2 OH                                 SO.sub.2  -n-C.sub.3 H.sub.7                                                             H        H      OCH.sub.3                                                                               CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 2h                                     __________________________________________________________________________      ##STR60##                                                                     R.sub.14                                                                               R.sub.15                                                                            R.sub.21                                                                          X    Y           m.p. (°C.)                             __________________________________________________________________________     Cl      H    H  CH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                  Br      H    H  CH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                      F       H    H  OCH.sub.3                                                                           CH.sub.2 SC.sub.2 H.sub.5                                 H       H    H  OCH.sub.3                                                                           CH.sub.2 OCO.sub.2 CH.sub.3                               Cl      3-Cl H  CH.sub.3                                                                            CH.sub.2 SCH.sub.3                                        Cl      H    H  OCH.sub.3                                                                           CH(OC.sub.2 H.sub.5).sub.2                                OCH.sub.3                                                                              H    H  CH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                         CH.sub.3                                                                               H    H  OCH.sub.3                                                                           CH.sub.2 OCO .sub.- i-C.sub.3 H.sub.7                     CH.sub.3                                                                               H    H  CH.sub.3                                                                            CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                        NO.sub.2                                                                               H    H  OCH.sub.3                                                                           CH(OC.sub.2 H.sub.5).sub.2                                CH.sub.3                                                                               4-F  H  OCH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                  Cl      6-NO.sub.2                                                                          H  OCH.sub.3                                                                           CH.sub.2 OCOCH.sub.3                                      NO.sub.2                                                                               H    CH.sub.3                                                                          CH.sub.3                                                                            CH.sub.2 OCOC.sub.2 H.sub.5                               Cl      6-F  H  CH.sub.3                                                                            CH.sub.2 OCO.sub.2  -n-C.sub.3 H.sub.7                    NO.sub.2                                                                               4-Cl CH.sub.3                                                                          CH.sub.3                                                                            CH.sub.2 SCH.sub.3                                        Cl      5-OCH.sub.3                                                                         H  OCH.sub.3                                                                           CH.sub.2 SC.sub.2 H.sub.5                                 F       H    H  CH.sub.3                                                                            CH(SCH(CH.sub.3)CH.sub.2 S)                               H       H    H  CH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                SO.sub.2 N(CH.sub.3).sub.2                                                             H    H  OCH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                  SO.sub.2 N(CH.sub.3).sub.2                                                             H    H  OCH.sub.3                                                                           CH.sub.2 OCONHCH.sub.3                                    OCH.sub.3                                                                              H    H  CH.sub.3                                                                            CH.sub.2 OCONH -n-C.sub.3 H.sub.7                         OSO.sub.2 CH.sub.3                                                                     H    H  CH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                      SO.sub. 2  -n-C.sub.3 H.sub.7                                                          H    H  OCH.sub.3                                                                           CH(OC.sub.2 H.sub.5).sub.2                                Cl      H    H  OCH.sub.3                                                                           CH.sub.2 SO.sub.2 CH.sub.3                                H       H    H  OCH.sub.3                                                                           CH(SCH.sub.3).sub.2                                       OCH.sub.3                                                                              H    H  CH.sub.3                                                                            C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                         SO.sub.2 CH.sub.3                                                                      H    H  CH.sub.3                                                                            CH(C.sub.2 H.sub.5)SO.sub.2 CH.sub.3                      NO.sub.2                                                                               H    H  CH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                       NO.sub.2                                                                               H    H  CH.sub.3                                                                            CH.sub.2 S(O)CH.sub.3                                     __________________________________________________________________________

                                      TABLE 3a                                     __________________________________________________________________________      ##STR61##                                                                     R.sub.14                                                                              R.sub.15                                                                             R.sub.21                                                                          X      Y         m.p. (°C.)                             __________________________________________________________________________     Cl     H     H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                                                      177-178° d                             Br     H     H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                     F      H     H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     H      H     H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     Cl     H     H  Cl     CH(OCH.sub.3).sub.2                                     Cl     3-Cl  H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                     Cl     H     H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                                                      156-175° d                             OCH.sub.3                                                                             H     H  CH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                                     CH.sub.3                                                                              H     H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     Br     H     H  Cl     CH(OCH.sub.3).sub.2                                     CH.sub.3                                                                              H     H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                     NO.sub.2                                                                              H     H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     CH.sub.3                                                                              4-F   H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     Cl     6-NO.sub.2                                                                           H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     NO.sub.2                                                                              H     H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                     NO.sub.2                                                                              H     H  Cl     CH(OCH.sub.3).sub.2                                     Cl     6-F   CH.sub.3                                                                          CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                     NO.sub.2                                                                              4-Cl  H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                     Cl     5-OCH.sub.3                                                                          H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     F      H     H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                     H      H     H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                     SO.sub.2 N(CH.sub.3).sub.2                                                            H     H  OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 N(CH.sub.3).sub.2                                                            H     H  OCH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                     OCH.sub.3                                                                             H     H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                     OSO.sub.2 CH.sub.3                                                                    H     H  CH.sub.3                                                                              CH(OCH.sub.3).sub.2                                     Cl     H     H  CH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                            NO.sub.2                                                                              H     H  CH.sub.3                                                                              C(C.sub.2 H.sub.5)(OCH.sub.3).sub.2                     OCH.sub.3                                                                             H     H  CH.sub.3                                                                              C(C.sub.2 H.sub.5)(OCH.sub.3).sub.2                     Br     H     H  OCH.sub.3                                                                             C(C.sub.2 H.sub.5)(OCH.sub.3).sub.2                     __________________________________________________________________________

                  TABLE 3b                                                         ______________________________________                                          ##STR62##                                                                                                        m.p.                                        R.sub.14   R.sub.15 R.sub.21                                                                              X       Y(° C.)                              ______________________________________                                         Cl         H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                               Br         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               F          H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               H          H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               Cl         3-Cl     H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                               OCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               CH.sub.3   H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               CH.sub.3   H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               NO.sub.2   H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               CH.sub.3   4-F      H      OCH.sub.3                                                                              CH.sub.2 OTHP                               Cl         6-NO.sub.2                                                                              H      OCH.sub.3                                                                              CH.sub.2 OTHP                               NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         6-F      H      CH.sub.3                                                                               CH.sub.2 OTHP                               NO.sub.2   4-Cl     H      CH.sub.3                                                                               CH.sub.2 OTHP                               Cl         5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OTHP                               F          H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                               H          H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                               SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               OCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               OSO.sub.2 CH.sub.3                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                               SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               O -n-C.sub.3 H.sub.7                                                                      H        H      CH.sub.3                                                                               CH.sub.2 OTHP                               ______________________________________                                    

                  TABLE 3c                                                         ______________________________________                                          ##STR63##                                                                     R.sub.14 R.sub.15 R.sub.21                                                                              X       Y      m.p.(° C.)                      ______________________________________                                         Cl       H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                   Br       H        H      CH.sub.3                                                                               CH.sub.2 OH                                   F        H        H      OCH.sub.3                                                                              CH.sub.2 OH                                   H        H        H      OCH.sub.3                                                                              CH.sub.2 OH                                   Cl       3-Cl     H      CH.sub.3                                                                               CH.sub.2 OH                                   Cl       H        H      OCH.sub.3                                                                              CH.sub.2 OH                                   OCH.sub.3                                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                   CH.sub.3 H        H      OCH.sub.3                                                                              CH.sub.2 OH                                   CH.sub.3 H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                   NO.sub.2 H        H      OCH.sub.3                                                                              CH.sub. 2 OH                                  CH.sub.3 4-F      H      OCH.sub.3                                                                              CH.sub.2 OH                                   Cl       6-NO.sub.2                                                                              H      OCH.sub.3                                                                              CH.sub.2 OH                                   NO.sub.2 H        H      CH.sub.3                                                                               CH.sub.2 OH                                   Cl       6-F      H      CH.sub.3                                                                               CH.sub.2 OH                                   NO.sub.2 4-Cl     H      CH.sub.3                                                                               CH.sub.2 OH                                   Cl       5-OCH.sub.3                                                                             H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                   F        H        H      CH.sub.3                                                                               CH.sub.2 OH                                   H        H        H      CH.sub.3                                                                               CH.sub.2 OH                                   SO.sub.2 N(CH.sub.3).sub.2                                                              H        CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                                   SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                              CH.sub.2 OH                                   OCH.sub.3                                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                   OSO.sub.2 CH.sub.3                                                                      H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                   SO.sub.2 H-n-C.sub.3 H.sub.7                                                                     H      OCH.sub.3                                                                              CH.sub.2 OH                                   ______________________________________                                    

                                      TABLE 3d                                     __________________________________________________________________________      ##STR64##                                                                     R.sub.14                                                                              R.sub.15                                                                            R.sub.21                                                                          X     Y            m.p. (° C.)                           __________________________________________________________________________     Cl     H    H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                                                    180-182° d                            Br     H    H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                      F      H    H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                                 H      H    CH.sub.3                                                                          OCH.sub.3                                                                            CH.sub.2 OCO.sub.2 CH.sub.3                               Cl     3-Cl H  CH.sub.3                                                                             CH.sub.2 SCH.sub.3                                        Cl     H    H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                OCH.sub.3                                                                             H    H  CH.sub.2 CH.sub.3                                                                    CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                         CH.sub.3                                                                              H    H  OCH.sub.3                                                                            CH.sub.2 OCO - i-C.sub.3 H.sub.7                          CH.sub.3                                                                              H    H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                        NO.sub.2                                                                              H    H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                CH.sub.3                                                                              4-F  H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                  Cl     6-NO.sub.2                                                                          H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                      NO.sub.2                                                                              H    H  CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                               Cl     6-F  H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2  -n-C.sub.3 H.sub.7                    NO.sub.2                                                                              4-Cl H  CH.sub.3                                                                             CH.sub.2 SCH.sub.3                                        Cl     5-OCH.sub.3                                                                         H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                                 F      H    CH.sub.3                                                                          CH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2 O)                               H      H    H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                                SO.sub.2 N(CH.sub.3).sub.2                                                            H    H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                  SO.sub.2 N(CH.sub.3).sub.2                                                            H    H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OCONHCH.sub.3                                    OCH.sub.3                                                                             H    H  CH.sub.3                                                                             CH.sub.2 OCONH -n-C.sub.3 H.sub.7                         OSO.sub.2 CH.sub.3                                                                    H    H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                      SO.sub.2  -n-C.sub.3 H.sub.7                                                          H    H  OCH.sub. 3                                                                           CH(OC.sub.2 H.sub.5).sub.2                                Cl     H    H  OCH.sub.3                                                                            CH(CH.sub.3)SCH.sub.3                                     Br     H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.2 CH.sub.2 CH.sub.2 O)                F      H    H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                                OCH.sub.3                                                                             H    H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                       OCH.sub.3                                                                             H    H  CH.sub.3                                                                             CH.sub.2 S(O)CH.sub.2 CH.sub.3                            __________________________________________________________________________

                                      TABLE 3e                                     __________________________________________________________________________      ##STR65##                                                                     R.sub.14                                                                              R.sub.15                                                                            R.sub.21                                                                          X     Y          m.p. (°C.)                              __________________________________________________________________________     Cl     H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                       Br     H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                       F      H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                       H      H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                       Cl     3-Cl H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                       Cl     H    H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                       OCH.sub.3                                                                             H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                       CH.sub.3                                                                              H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                       CH.sub.3                                                                              H    H  CH.sub.3                                                                             CH(OCH.sub. 3).sub.2                                      NO.sub.2                                                                              H    H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                       CH.sub.3                                                                              4-F  CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                       Cl     6-NO.sub.2                                                                          H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                       NO.sub.2                                                                              H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                       Cl     6-F  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                       NO.sub.2                                                                              4-Cl H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                       Cl     5-OCH.sub.3                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                       F      H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                       H      H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                       SO.sub.2 N(CH.sub.3).sub.2                                                            H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                       SO.sub.2 N(CH.sub.3).sub.2                                                            H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                       OCH.sub.3                                                                             H    H  CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                       OSO.sub.2 CH.sub.3                                                                    H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                       SO.sub.2  -n-C.sub.3 H.sub.7                                                          H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                       SO.sub.2 N(CH.sub.3).sub.2                                                            H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                              Cl     H    H  OCH.sub. 3                                                                           C(CH.sub.3)(OCH.sub.3).sub.2                              NO.sub.2                                                                              H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                              OCH.sub.3                                                                             H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                              F      H    H  CH.sub.3                                                                             C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2                     __________________________________________________________________________

                  TABLE 3f                                                         ______________________________________                                          ##STR66##                                                                                                               m.p.                                 R.sub.14  R.sub.15 R.sub.21                                                                              X       Y       (° C.)                        ______________________________________                                         Cl        H        CH.sub.3                                                                              CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                                Br        H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                F         H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                H         H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                Cl        3-Cl     H      CH.sub.3                                                                               CH.sub.2 OTHP                                Cl        H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                OCH.sub.3 H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                CH.sub.3  H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                CH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                NO.sub.2  H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                CH.sub.3  4-F      H      OCH.sub.3                                                                              CH.sub.2 OTHP                                Cl        6-NO.sub.2                                                                              H      OCH.sub.3                                                                              CH.sub.2 OTHP                                NO.sub.2  H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                Cl        6-F      H      CH.sub.3                                                                               CH.sub.2 OTHP                                NO.sub.2  4-Cl     H      CH.sub.3                                                                               CH.sub.2 OTHP                                Cl        5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OTHP                                F         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                H         H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                SO.sub.2 N(CH.sub.3).sub.2                                                               H        CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OTHP                                SO.sub.2 N(CH.sub.3).sub.2                                                               H        H      OCH.sub.3                                                                              CH.sub.2 OTHP                                OCH.sub.3 H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                OSO.sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OTHP                                SO.sub.2  -n-C.sub.3 H.sub.7                                                             H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                ______________________________________                                    

                  TABLE 3g                                                         ______________________________________                                          ##STR67##                                                                     R.sub.14 R.sub.15 R.sub.21                                                                              X       Y      m.p.(° C.)                      ______________________________________                                         Cl       H        H      CH.sub.3                                                                               CH.sub.2 OH                                   Br       H        H      CH.sub.3                                                                               CH.sub.2 OH                                   F        H        H      OCH.sub.3                                                                              CH.sub.2 OH                                   H        H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                   Cl       3-Cl     H      CH.sub.3                                                                               CH.sub.2 OH                                   Cl       H        H      OCH.sub.3                                                                              CH.sub.2 OH                                   OCH.sub.3                                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                   CH.sub.3 H        H      OCH.sub.3                                                                              CH.sub.2 OH                                   CH.sub.3 H        H      CH.sub.3                                                                               CH.sub.2 OH                                   NO.sub.2 H        H      OCH.sub.3                                                                              CH.sub.2 OH                                   CH.sub.3 4-F      H      OCH.sub.3                                                                              CH.sub.2 OH                                   Cl       6-NO.sub.2                                                                              H      OCH.sub.3                                                                              CH.sub.2 OH                                   NO.sub.2 H        H      CH.sub.3                                                                               CH.sub.2 OH                                   Cl       6-F      H      CH.sub.3                                                                               CH.sub.2 OH                                   NO.sub.2 4-Cl     H      CH.sub.3                                                                               CH.sub.2 OH                                   Cl       5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                   F        H        H      CH.sub.3                                                                               CH.sub.2 OH                                   H        H        H      CH.sub.3                                                                               CH.sub.2 OH                                   SO.sub.2 N(CH.sub.3).sub.2                                                              H        H      OCH.sub.3                                                                              CH.sub.2 OH                                   SO.sub.2 N(CH.sub.3).sub.2                                                              H        CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                                   OCH.sub.3                                                                               H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                   OSO.sub.2 CH.sub.3                                                                      H        H      CH.sub.3                                                                               CH.sub.2 OH                                   SO.sub.2 H-n-C.sub.3 H.sub.7                                                                     H      OCH.sub.3                                                                              CH.sub.2 OH                                   ______________________________________                                    

                                      TABLE 3h                                     __________________________________________________________________________      ##STR68##                                                                     R.sub.14                                                                              R.sub.15                                                                            R.sub.21                                                                          X     Y           m.p. (° C.)                            __________________________________________________________________________     Cl     H    CH.sub.3                                                                          CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                                  Br     H    H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                      F      H    H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 SC.sub.2 H.sub.5                                 H      H    H  OCH.sub.3                                                                            CH.sub.2 OCO.sub.2 CH.sub.3                               Cl     3-Cl H  CH.sub.3                                                                             CH.sub.2 SCH.sub.3                                        Cl     H    H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                OCH.sub.3                                                                             H    H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                         CH.sub.3                                                                              H    H  OCH.sub. 3                                                                           CH.sub.2 OCO -n-C.sub.3 H.sub.7                           CH.sub.3                                                                              H    H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                        NO.sub.2                                                                              H    H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                CH.sub.3                                                                              4-F  H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                  Cl     6-NO.sub.2                                                                          H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                      NO.sub.2                                                                              H    H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OCOC.sub.2 H.sub.5                               Cl     6-F  H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2  -n-C.sub.3 H.sub.7                    NO.sub.2                                                                              4-Cl H  CH.sub.3                                                                             CH.sub.2 SCH.sub.3                                        Cl     5-OCH.sub.3                                                                         H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                                 F      H    H  CH.sub.3                                                                             CH(SCH(CH.sub.3)CH.sub.2 S)                               H      H    H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                                SO.sub.2 N(CH.sub.3).sub.2                                                            H    CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                  SO.sub.2 N(CH.sub.3).sub.2                                                            H    H  OCH.sub.3                                                                            CH.sub.2 OCONHCH.sub.3                                    OCH.sub.3                                                                             H    H  CH.sub.3                                                                             CH.sub.2 OCONH -n-C.sub.3 H.sub.7                         OSO.sub.2 CH.sub.3                                                                    H    H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                      SO.sub.2  -n-C.sub.3 H.sub.7                                                          H    H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                                NO.sub.2                                                                              H    H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                         Cl     H    H  OCH.sub.3                                                                            C(CH.sub.3)(SCH.sub.2 CH.sub.2 S)                         OSO.sub.2 CH.sub.3                                                                    H    H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                                SO.sub.2  -n-C.sub.3 H.sub.7                                                          H    H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                                CH.sub.3                                                                              H    H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                                Br     H    H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                                Br     H    H  CH.sub.3                                                                             CH(CH.sub.3)(S(O)CH.sub.3)                                __________________________________________________________________________

                  TABLE 4a                                                         ______________________________________                                          ##STR69##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         Cl         H        H      CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.3).sub.2                         CO.sub.2 CH.sub.3                                                                         H        H      Cl      CH(OCH.sub.3).sub.2                         Cl         H        CH.sub.3                                                                              OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                         H          H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                         CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         NO.sub.2   H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         NO.sub.2   6-Br     H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         Cl         4-Cl     H      Cl      CH(OCH.sub.3).sub.2                         CF.sub.3   H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                         Cl         6-CH.sub.3                                                                              CH.sub.3                                                                              OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                         C.sub.2 H.sub.5                                                                           H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                         SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                         SO.sub.2  -n-C.sub.4 H.sub.9                                                              H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                         SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         SO.sub.2  -n-C.sub.3 H.sub.7                                                              H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         SO.sub.2  .sub.- i-C.sub.3 H.sub.7                                                        H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                         SCH.sub.3  H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                         SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                         S(O).sub.2 (CH.sub.2).sub.3 CH.sub.3                                                      H        H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                         Cl         H        H      CH.sub.3                                                                               C(CH.sub.3)(OCH.sub.3).sub.2                NO.sub.2   H        H      OCH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                 CO.sub.2 C.sub.2 H.sub.5                                                                  H        H      OCH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      OCH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                 ______________________________________                                    

                  TABLE 4b                                                         ______________________________________                                          ##STR70##                                                                                                             m.p.                                   R.sub.16   R.sub.17 R.sub.21 X  Y       (°C.)                           ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        HCH.sub.3   CH.sub.2 OTHP                                  Cl         H        HCH.sub.2 CH.sub.3                                                                         CH.sub.2 OTHP                                  Cl         H        HOCH.sub.3  CH.sub.2 OTHP                                  H          H        HOCH.sub.3  CH.sub.2 OTHP                                  CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      HCH.sub.3   CH.sub.2 OTHP                                  CO.sub.2 CH(CH.sub.3).sub.2                                                               H        HCH.sub.3   CH.sub.2 OTHP                                  NO.sub.2   H        HCH.sub.3   CH.sub.2 OTHP                                  NO.sub.2   6-Br     HCH.sub.3   CH.sub.2 OTHP                                  Cl         4-Cl     HOCH.sub.3  CH.sub.2 OTHP                                  CF.sub.3   H        HOCH.sub.3  CH.sub.2 OTHP                                  Cl         6-CH.sub.3                                                                              HOCH.sub.3  CH.sub.2 OTHP                                  C.sub.2 H.sub.5                                                                           H        H CH.sub.3  CH.sub.2 OTHP                                  CH(CH.sub.3).sub.2                                                                        H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             HOCH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         6-F      HOCH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 N(CH.sub.3).sub.2                                                                H        CH.sub.3 OCH.sub.3                                                                         CH.sub.2 OTHP                                  SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 -i-C.sub.3 H.sub.7                                                               H        HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OTHP                                  SCH.sub.3  H        HCH.sub.3   CH.sub.2 OTHP                                  S(O).sub.2 CH.sub.3                                                                       H        HCH.sub.3   CH.sub.2 OTHP                                  SCH.sub.2 CH.sub.3                                                                        H        HOCH.sub.3  CH.sub.2 OTHP                                  S(O).sub.2 -n-C.sub.4 H.sub.9                                                             H        HOCH.sub.3  CH.sub.2 OTHP                                  ______________________________________                                    

                  TABLE 4c                                                         ______________________________________                                          ##STR71##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                                 H          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.3                                                                               CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         4-Cl     H      OCH.sub.3                                                                              CH.sub.2 OH                                 CF.sub.3   H        H      OCH.sub. 3                                                                             CH.sub.2 OH                                 Cl         6-CH.sub.3                                                                              CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                                 C.sub.2 H.sub.5                                                                           H        H      CH.sub.3                                                                               CH.sub.2 OH                                 CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -i-C.sub.3 H.sub.7                                                               H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SCH.sub.3  H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 S(O).sub.2 H-n-C.sub.4 H.sub.9                                                                     H      OCH.sub.3                                                                              CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 4d                                     __________________________________________________________________________      ##STR72##                                                                     R.sub.16  R.sub.17                                                                             R.sub.21                                                                           X      Y            m.p. (°C.)                      __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                        H     CH.sub.3                                                                           CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                                Cl        H     H   CH.sub.2 CH.sub.3                                                                     CH(OC.sub.2 H.sub.5).sub.2                          Cl        H     H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  H         H     H   OCH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                              CO.sub.2 CH(CH.sub.3).sub.2                                                              5-F   H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                         CO.sub.2 CH(CH.sub.3).sub.2                                                              H     H   CH.sub.3                                                                              CH.sub.2 SC.sub.2 H.sub.5                           NO.sub.2  H     H   CH.sub.3                                                                              CH(SCH.sub.2 CH.sub.2 S)                            NO.sub.2  6-Br  H   CH.sub.3                                                                              CH.sub.2 OCOC.sub.2 H.sub.5                         Cl        4-Cl  H   OCH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                   CF.sub.3  H     CH.sub.3                                                                           OCH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2)                           Cl        6-CH.sub.3                                                                           H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  C.sub.2 H.sub.5                                                                          H     H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                                CH(CH.sub.3).sub.2                                                                       H     H   CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3).sub.2                       SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            SO.sub.2 CH.sub.3                                                                        4-OCH.sub.3                                                                          H   OCH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                SO.sub.2 CH.sub.3                                                                        6-F   H   OCH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                           SO.sub.2 -n-C.sub.4 H.sub.9                                                              H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   OCH.sub.2 CH.sub.3                                                                    CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7               SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                        H     H   CH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H     H   CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3)(  -n-C.sub.3 H.sub.7)       SO.sub.2 -n-C.sub.3 H.sub.7                                                              H     H   CH.sub.3                                                                              CH.sub. 2 OCO -i-C.sub.3 H.sub.7                    SO.sub.2 -i-C.sub.3 H.sub.7                                                              H     H   OCH.sub.3                                                                             CH.sub.2 OCONH( .sub.-n-C.sub.3 H.sub.7)            SCH.sub.3 H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          S(O).sub.2 CH.sub.3                                                                      H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SCH.sub.2 CH.sub.3                                                                       H     H   OCH.sub.3                                                                             CH.sub.2 OCO.sub.2 -i-C.sub.3 H.sub.7               S(O).sub.2 -n-C.sub.4 H.sub.9                                                            H     CH.sub.3                                                                           OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  Cl        H     H   OCH.sub.3                                                                             CH(SCH.sub.2 CH.sub.3).sub.2                        CH.sub.3  H     H   OCH.sub.3                                                                             C(CH.sub.3)(OCH.sub. 2 CH.sub.2 O)                  SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   OCH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                          SCH.sub.3 H     H   CH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                 SCH.sub.3 H     H   OCH.sub.3                                                                             CH.sub.2 S(O)CH.sub.3                               __________________________________________________________________________

                  TABLE 4e                                                         ______________________________________                                          ##STR73##                                                                                                             m.p.                                   R.sub.16   R.sub.17 R.sub.21X   Y       (°C.)                           ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        HCH.sub.3   CH(OCH.sub.3).sub.2                            Cl         H        HCH.sub.2 CH.sub.3                                                                         CH(OCH.sub.3).sub.2                            Cl         H        CH.sub.3OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                            H          H        HOCH.sub.3  CH(OCH.sub.3).sub.2                            CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      HCH.sub.3   CH(OCH.sub.3).sub.2                            CO.sub.2 CH(CH.sub.3).sub.2                                                               H        HCH.sub.3   CH(OCH.sub.3).sub.2                            NO.sub.2   H        HCH.sub.3   CH(OCH.sub.3).sub.2                            NO.sub.2   6-Br     HCH.sub.3   CH(OCH.sub.3).sub.2                            CF.sub.3   H        HOCH.sub. 3 CH(OCH.sub.3).sub.2                            Cl         6-CH.sub.3                                                                              HOCH.sub.3  CH(OCH.sub.3).sub.2                            C.sub.2 H.sub.5                                                                           H        HCH.sub.3   CH(OCH.sub.3).sub.2                            CH(CH.sub.3).sub.2                                                                        H        HCH.sub.3   CH(OCH.sub.3).sub.2                            SO.sub.2 CH.sub.3                                                                         H        HCH.sub.3   CH(OCH.sub.3).sub.2                            SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             HOCH.sub.2 CH.sub.3                                                                        CH(OCH.sub.3).sub.2                            SO.sub.2 CH.sub.3                                                                         6-F      HOCH.sub.3  CH(OCH.sub.3).sub.2                            SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        HCH.sub.3   CH(OCH.sub.3).sub.2                            SO.sub.2 N(CH.sub.3).sub.2                                                                H        HOCH.sub.3  CH(OCH.sub.3).sub.2                            SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        HCH.sub.3   CH(OCH.sub.3).sub.2                            SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        HCH.sub.3   CH(OCH.sub.3).sub.2                            SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        HCH.sub.3   CH(OCH.sub.3).sub.2                            SO.sub.2 -i-C.sub.3 H.sub.7                                                               H        HOCH.sub.2 CH.sub.3                                                                        CH(OCH.sub.3).sub.2                            SCH.sub.3  H        CH.sub.3CH.sub.3                                                                           CH(OCH.sub.3).sub.2                            S(O).sub.2 CH.sub.3                                                                       H        HCH.sub.3   CH(OCH.sub.3).sub. 2                           SCH.sub.2 CH.sub.3                                                                        H        HOCH.sub.3  CH(OCH.sub.3).sub.2                            S(O).sub.2 (CH.sub.2).sub.3 CH.sub.3                                                      H        HOCH.sub.3  CH(OCH.sub.3).sub.2                            CF.sub.3   H        HCH.sub.3   C(CH.sub.3)(OCH.sub. 3).sub.2                  Cl         H        HOCH.sub.3  C(CH.sub.3)(OCH.sub. 3).sub.2                  NO.sub.2   H        HOCH.sub.3  C(CH.sub.3)(OCH.sub. 3).sub.2                  SO.sub.2 CH.sub.2 CH.sub.3                                                                H        HOCH.sub.3  C(CH.sub.3)(OCH.sub. 3).sub.2                  ______________________________________                                    

                  TABLE 4f                                                         ______________________________________                                          ##STR74##                                                                                                             m.p.                                   R.sub.16   R.sub.17 R.sub.21 X  Y       (°C.)                           ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        HCH.sub.3   CH.sub.2 OTHP                                  Cl         H        HCH.sub.3   CH.sub.2 OTHP                                  Cl         H        HOCH.sub.3  CH.sub.2 OTHP                                  H          H        HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OTHP                                  CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      HCH.sub.3   CH.sub.2 OTHP                                  CO.sub.2 CH(CH.sub.3).sub.2                                                               H        HCH.sub.3   CH.sub.2 OTHP                                  NO.sub.2   H        HCH.sub.3   CH.sub.2 OTHP                                  NO.sub.2   6-Br     HCH.sub.3   CH.sub.2 OTHP                                  Cl         4-Cl     HOCH.sub.3  CH.sub.2 OTHP                                  CF.sub.3   H        CH.sub.3 OCH.sub.3                                                                         CH.sub.2 OTHP                                  Cl         6-CH.sub.3                                                                              HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OTHP                                  C.sub.2 H.sub.5                                                                           H        HCH.sub.3   CH.sub.2 OTHP                                  CH(CH.sub.3).sub.2                                                                        H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             HOCH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         6-F      HOCH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 N(CH.sub.3).sub.2                                                                H        HOCH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 -i-C.sub.3 H.sub.7                                                               H        HOCH.sub.3  CH.sub.2 OTHP                                  SCH.sub.3  H        HCH.sub.3   CH.sub.2 OTHP                                  S(O).sub.2 CH.sub.3                                                                       H        HCH.sub.2 CH.sub.3                                                                         CH.sub.2 OTHP                                  SCH.sub.2 CH.sub.3                                                                        H        HOCH.sub.3  CH.sub.2 OTHP                                  S(O).sub.2 -n-C.sub.4 H.sub.9                                                             H        HOCH.sub.3  CH.sub.2 OTHP                                  ______________________________________                                    

                  TABLE 4g                                                         ______________________________________                                          ##STR75##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 H          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         4-Cl     H      OCH.sub.3                                                                              CH.sub. 2 OH                                CF.sub.3   H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 Cl         6-CH.sub.3                                                                              H      OCH.sub.3                                                                              CH.sub.2 OH                                 C.sub.2 H.sub.5                                                                           H        H      CH.sub.3                                                                               CH.sub.2 OH                                 CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -i-C.sub.3 H.sub.7                                                               H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OH                                 S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 S(O).sub.2 -n-C.sub.4 H.sub.9                                                             H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 4h                                     __________________________________________________________________________      ##STR76##                                                                     R.sub.16  R.sub.17                                                                             R.sub.21                                                                           X      Y            m.p. (°C.)                      __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                        H     H   CH.sub.2 CH.sub.3                                                                     CH.sub.2 OCOCH.sub.3                                Cl        H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          Cl        H     H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  H         H     H   OCH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                              CO.sub.2 CH(CH.sub.3).sub.2                                                              5-F   H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                         CO.sub.2 CH(CH.sub.3).sub.2                                                              H     H   CH.sub.3                                                                              CH.sub.2 SC.sub.2 H.sub.5                           NO.sub.2  H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            NO.sub.2  6-Br  CH.sub.3                                                                           CH.sub.3                                                                              CH.sub.2 OCOC.sub.2 H.sub.5                         Cl        4-Cl  H   OCH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                   CF.sub.3  H     H   OCH.sub.2 CH.sub.3                                                                    CH(OCH(CH.sub.3)CH.sub.2)                           Cl        6-CH.sub.3                                                                           H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  C.sub.2 H.sub.5                                                                          H     H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                                CH(CH.sub.3).sub.2                                                                       H     H   CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3).sub.2                       SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            SO.sub.2 CH.sub.3                                                                        4-OCH.sub.3                                                                          H   OCH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                SO.sub.2 CH.sub.3                                                                        6-F   H   OCH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                           SO.sub.2 -n-C.sub.4 H.sub.9                                                              H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   OCH.sub.3                                                                             CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7               SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                        H     H   CH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H     CH.sub.3                                                                           CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3)( -n-C.sub.3 H.sub.7)        SO.sub.2 -n-C.sub.3 H.sub.7                                                              H     H   CH.sub.3                                                                              CH.sub.2 OCO -i-C.sub.3 H.sub.7                     SO.sub.2 -i-C.sub.3 H.sub.7                                                              H     H   OCH.sub.3                                                                             CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)                 SCH.sub.3 H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          S(O).sub.2 CH.sub.3                                                                      H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SCH.sub.2 CH.sub.3                                                                       H     H   OCH.sub.3                                                                             CH.sub.2 OCO.sub.2 -i-C.sub.3 H.sub.7               S(O).sub.2 -n-C.sub.4 H.sub.9                                                            H     H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  NO.sub.2  H     H   CH.sub.3                                                                              CH(CH.sub.3)(SCH.sub.3).sub.2                       Cl        H     H   CH.sub.3                                                                              CH(CH.sub.3)(SO.sub.2 CH.sub.3)                     CF.sub.3  H     H   CH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                          CO.sub.2 CH.sub.2 CH.sub.3                                                               H     H   CH.sub.3                                                                              CH(SCH.sub.3).sub.2                                 CO.sub.2 CH.sub.2 CH.sub.3                                                               H     H   OCH.sub.3                                                                             CH.sub.2 S(O)CH.sub.2 CH.sub.3                      CO.sub.2 CH.sub.2 CH.sub.3                                                               H     H   CH.sub.3                                                                              CH.sub.2 S(O)CH.sub.3                               __________________________________________________________________________

                  TABLE 5a                                                         ______________________________________                                          ##STR77##                                                                                                               m.p.                                 R.sub.16   R.sub.17                                                                               R.sub.21                                                                              X       Y       (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          Cl         H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          CO.sub.2 CH.sub.3                                                                         H       CH.sub.3                                                                              Cl      CH(OCH.sub.3).sub.2                          Cl         H       H      OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                          H          H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F     H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          CO.sub.2 CH(CH.sub.3).sub.2                                                               H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          NO.sub.2   H       H      CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.3).sub.2                          NO.sub.2   6-Br    H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          Cl         4-Cl    H      Cl      CH(OCH.sub.3).sub.2                          CF.sub.3   H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          Cl         6-CH.sub.3                                                                             H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          C.sub.2 H.sub.5                                                                           H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          CH(CH.sub.3).sub.2                                                                        H       H      CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.3).sub.2                          SO.sub.2 CH.sub.3                                                                         H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 CH.sub.3                                                                         4-      H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                                     OCH.sub.3                                                           SO.sub.2 CH.sub.3                                                                         6-F     H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2  -n-C.sub.4 H.sub.9                                                              H       CH.sub.3                                                                              CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 N(CH.sub.3).sub.2                                                                H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 -n-C.sub.3 H.sub.7                                                               H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 -i-C.sub.3 H.sub.7                                                               H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SCH.sub.3  H       H      CH.sub.3                                                                               CH(OCH.sub.3 ).sub.2                         S(O).sub.2 CH.sub.3                                                                       H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          CH.sub.2 CH.sub.3                                                                         H       H      CH.sub.3                                                                            C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2           SCH.sub.3  H       H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 NO.sub.2   H       H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 CO.sub.2 CH.sub.3                                                                         H       H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 SCH.sub.2 CH.sub.3                                                                        H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          S(O).sub.2 (CH.sub.2).sub.3 CH.sub.3                                                      H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          ______________________________________                                    

                  TABLE 5b                                                         ______________________________________                                          ##STR78##                                                                                                             m.p.                                   R.sub.16   R.sub.17 R.sub.21                                                                         X         Y       (°C.)                           ______________________________________                                         CO.sub.2 CH.sub.3                                                                         HH         CH.sub.3  CH.sub.2 OTHP                                  Cl         HH         CH.sub.3  CH.sub.2 OTHP                                  Cl         HH         OCH.sub.3 CH.sub.2 OTHP                                  H          HH         OCH.sub.3 CH.sub.2 OTHP                                  CO.sub.2 CH(CH.sub.3).sub.2                                                               5-FH       CH.sub.3  CH.sub.2 OTHP                                  CO.sub.2 CH(CH.sub.3).sub.2                                                               HH         CH.sub.2 CH.sub.3                                                                        CH.sub.2 OTHP                                  NO.sub.2   HH         CH.sub.3  CH.sub.2 OTHP                                  NO.sub.2   6-BrH      CH.sub.3  CH.sub.2 OTHP                                  Cl         4-ClH      OCH.sub.3 CH.sub.2 OTHP                                  CF.sub.3   HH         OCH.sub.3 CH.sub.2 OTHP                                  Cl         6-CH.sub.3 H                                                                              OCH.sub.3 CH.sub.2 OTHP                                  C.sub.2 H.sub.5                                                                           HH         CH.sub.3  CH.sub.2 OTHP                                  CH(CH.sub.3).sub.2                                                                        HCH.sub.3  CH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         HH         CH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3 H                                                                             OCH.sub.2 CH.sub.3                                                                       CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         6-FH       OCH.sub.3 CH.sub.2 OTHP                                  SO.sub.2 -n-C.sub.4 H.sub.9                                                               HH         CH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 N(CH.sub.3).sub.2                                                                HH         OCH.sub.3 CH.sub.2 OTHP                                  SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         HH         CH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             HH         CH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 -n-C.sub.3 H.sub.7                                                               HH         CH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 -i-C.sub.3 H.sub.7                                                               HH         OCH.sub.3 CH.sub.2 OTHP                                  SCH.sub.3  HH         CH.sub.3  CH.sub.2 OTHP                                  S(O).sub.2 CH.sub.3                                                                       HH         CH.sub.3  CH.sub.2 OTHP                                  SCH.sub.2 CH.sub.3                                                                        HH         OCH.sub. 3                                                                               CH.sub.2 OTHP                                  S(O).sub.2 -n-C.sub.4 H.sub.9                                                             HH         OCH.sub.3 CH.sub.2 OTHP                                  ______________________________________                                    

                  TABLE 5c                                                         ______________________________________                                          ##STR79##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 H          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.3                                                                               CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         4-Cl     H      OCH.sub.3                                                                              CH.sub.2 OH                                 CF.sub.3   H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 Cl         6-CH.sub.3                                                                              H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 C.sub.2 H.sub.5                                                                           H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                 CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -i-C.sub.3 H.sub.7                                                               H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OH                                 S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub. 3                                                                              CH.sub.2 OH                                 SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 S(O).sub.2 -n-C.sub.4 H.sub.9                                                             H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 ______________________________________                                    

                  TABLE 5d                                                         ______________________________________                                          ##STR80##                                                                                                               m.p.                                 R.sub.16   R.sub.17                                                                              R.sub.21                                                                              X       Y        (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H      H      CH.sub.3                                                                               CH.sub.2 OCOCH.sub.3                          Cl         H      CH.sub.3                                                                              CH.sub.3                                                                               CH(OC.sub.2 H.sub.5).sub.2                    Cl         H      H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 SCH.sub.3                            H          H      H      OCH.sub.3                                                                              CH.sub.2 OCONHCH.sub.3                        CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F    H      CH.sub.3                                                                               CH.sub.2 OCO.sub.2 CH.sub.3                   CO.sub.2 CH(CH.sub.3).sub.2                                                               H      H      CH.sub.3                                                                               CH.sub.2 SC.sub.2 H.sub.5                     NO.sub.2   H      H      CH.sub.3                                                                               CH(OCH.sub.2 CH.sub.2 O)                      NO.sub.2   6-Br   H      CH.sub.3                                                                               CH.sub.2 OCOC.sub.2 H.sub.5                   Cl         4-Cl   H      OCH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)              CF.sub.3   H      H      OCH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2)                      Cl         6-     H      OCH.sub.3                                                                              CH.sub.2 SCH.sub.3                                       CH.sub.3                                                            C.sub.2 H.sub.5                                                                           H      H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OCOCH.sub.3                          CH(CH.sub.3).sub.2                                                                        H      H      CH.sub.3                                                                               CH.sub.2 OCON(CH.sub.3).sub.2                 SO.sub.2 CH.sub.3                                                                         H      H      CH.sub.3                                                                               CH(OCH.sub.2 CH.sub.2 O)                      SO.sub.2 CH.sub.3                                                                         4-      H     OCH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                                     OCH.sub.3                                                           SO.sub.2 CH.sub.3                                                                         6-F    H      OCH.sub.3                                                                              CH.sub.2 SC.sub.2 H.sub.5                     SO.sub.2 -n-C.sub.4 H.sub.9                                                               H      H      CH.sub.3                                                                               CH(OC.sub.2 H.sub. 5).sub.2                   SO.sub.2 N(CH.sub.3).sub.2                                                                H      H      OCH.sub.3                                                                              CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7         SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H      H      CH.sub.3                                                                               CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2          SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H      H      CH.sub.3                                                                               CH.sub.2 OCON(CH.sub.3)( -n-                                                   C.sub.3 H.sub.7)                              SO.sub. 2 -n-C.sub.3 H.sub.7                                                              H      H      CH.sub.3                                                                               CH.sub.2 OCO -i-C.sub.3 H.sub.7               SO.sub.2 -i-C.sub.3 H.sub.7                                                               H      H      OCH.sub.3                                                                              CH.sub.2 OCONH( -n-                                                            C.sub.3 H.sub.7)                              SCH.sub.3  H      CH.sub.3                                                                              CH.sub.3                                                                               CH(OC.sub.2 H.sub.5).sub.2                    S(O).sub.2 CH.sub.3                                                                       H      H      CH.sub.3                                                                               CH(OC.sub.2 H.sub.5).sub.2                    SCH.sub.2 CH.sub.3                                                                        H      H      OCH.sub.3                                                                              CH.sub.2 OCO.sub.2 -i-C.sub.3 H.sub.7         S(O).sub.2 -n-C.sub.4 H.sub.9                                                             H      H      OCH.sub.3                                                                              CH.sub.2 SCH.sub.3                            CO.sub.2 CH.sub.2 CH.sub.3                                                                H      H      CH.sub.3                                                                               C(CH.sub.3)(OC.sub.2 H.sub.5).sub.2           CF.sub.3   H      H      CH.sub.3                                                                               CH(CH.sub.3)SC.sub.2 H.sub.5                  SO.sub.2 CH.sub.3                                                                         H      H      CH.sub.3                                                                               CH.sub.2 SO.sub.2 CH.sub.3                    SO.sub.2 CH.sub.3                                                                         H      H      CH.sub.3                                                                               CH.sub.2 S(O)CH.sub.3                         SO.sub.2 CH.sub.3                                                                         H      H      CH.sub.3                                                                               CH(CH.sub.3)(S(O)CH.sub.3)                    ______________________________________                                    

                  TABLE 5e                                                         ______________________________________                                          ##STR81##                                                                                                               m.p.                                 R.sub.16   R.sub.17                                                                               R.sub.21                                                                              X       Y       (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          Cl         H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          Cl         H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          H          H       CH.sub.3                                                                              OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F     H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          CO.sub.2 CH(CH.sub.3).sub.2                                                               H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          NO.sub.2   H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          NO.sub.2   6-Br    H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          CF.sub.3   H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          Cl         6-CH.sub.3                                                                             H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          C.sub.2 H.sub.5                                                                           H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          CH(CH.sub.3).sub.2                                                                        H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 CH.sub.3                                                                         H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 CH.sub.3                                                                         4-      H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                                     OCH.sub.3                                                           SO.sub.2 CH.sub.3                                                                         6-F     H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 -n-C.sub.4 H.sub.9                                                               H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 N(CH.sub.3).sub.2                                                                H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 N(C.sub.2 H.sub.5 ).sub.2                                                        H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H       H      CH.sub.2 CH.sub.3                                                                      CH(OCH.sub.3).sub.2                          SO.sub.2 -n-C.sub.3 H.sub.7                                                               H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SO.sub.2  -i-C.sub.3 H.sub.7                                                              H       H      OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SCH.sub.3  H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          S(O).sub. 2 CH.sub.3                                                                      H       H      CH.sub.3                                                                               CH(OCH.sub.3).sub.2                          SCH.sub.2 CH.sub.3                                                                        H       H      OCH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                          S(O).sub.2 (CH.sub.2).sub.3 CH.sub.3                                                      H       CH.sub.3                                                                              OCH.sub.3                                                                              CH(OCH.sub.3).sub.2                          SO.sub.2 CH.sub.2 CH.sub.3                                                                H       H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 CH.sub.3   H       H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 CO.sub.2 CH.sub.3                                                                         H       H      OCH.sub.3                                                                              C(CH.sub.3)(OCH.sub.3).sub.2                 ______________________________________                                    

                  TABLE 5f                                                         ______________________________________                                          ##STR82##                                                                                                             m.p.                                   R.sub.16   R.sub.17 R.sub.21                                                                         X         Y       (°C.)                           ______________________________________                                         CO.sub.2 CH.sub.3                                                                         HH         CH.sub.3  CH.sub.2 OTHP                                  Cl         HH         CH.sub.3  CH.sub.2 OTHP                                  Cl         HH         OCH.sub.2 CH.sub.3                                                                       CH.sub.2 OTHP                                  H          HH         OCH.sub.3 CH.sub.2 OTHP                                  CO.sub.2 CH(CH.sub.3).sub.2                                                               5-FH       CH.sub.3  CH.sub.2 OTHP                                  CO.sub.2 CH(CH.sub.3).sub.2                                                               HH         CH.sub.3  CH.sub.2 OTHP                                  NO.sub.2   HH         CH.sub.3  CH.sub.2 OTHP                                  NO.sub.2   6-BrH      CH.sub.3  CH.sub.2 OTHP                                  Cl         4-ClH      OCH.sub.3 CH.sub.2 OTHP                                  CF.sub.3   HCH.sub.3  OCH.sub.3 CH.sub.2 OTHP                                  Cl         6-CH.sub.3 H                                                                              OCH.sub.3 CH.sub.2 OTHP                                  C.sub.2 H.sub.5                                                                           HH         CH.sub.3  CH.sub.2 OTHP                                  CH(CH.sub.3).sub.2                                                                        HH         CH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         HH         CH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3 H                                                                             OCH.sub.3 CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         6-FH       OCH.sub.3 CH.sub.2 OTHP                                  SO.sub.2 -n-C.sub.4 H.sub.9                                                               HH         CH.sub.2 CH.sub.3                                                                        CH.sub.2 OTHP                                  SO.sub.2 N(CH.sub.3).sub.2                                                                HH         OCH.sub.3 CH.sub.2 OTHP                                  SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         HH         CH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             HH         CH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 -n-C.sub.3 H.sub.7                                                               HH         CH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 -i-C.sub.3 H.sub.7                                                               HH         OCH.sub.3 CH.sub.2 OTHP                                  SCH.sub.3  HH         CH.sub.3  CH.sub.2 OTHP                                  S(O).sub.2 CH.sub.3                                                                       HH         CH.sub.3  CH.sub.2 OTHP                                  SCH.sub.2 CH.sub.3                                                                        HH         OCH.sub.3 CH.sub.2 OTHP                                  S(O).sub.2 -n-C.sub.4 H.sub.9                                                             HH         OCH.sub.3 CH.sub.2 OTHP                                  ______________________________________                                    

                  TABLE 5g                                                         ______________________________________                                          ##STR83##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 H          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.3                                                                               CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         4-Cl     H      OCH.sub.3                                                                              CH.sub. 2 OH                                CF.sub.3   H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 Cl         6-CH.sub.3                                                                              H      OCH.sub.3                                                                              CH OH                                       C.sub.2 H.sub.5                                                                           H        H      CH.sub.3                                                                               CH.sub.2 OH                                 CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         4-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -i-C.sub.3 H.sub.7                                                               H        CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OH                                 SCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OH                                 S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SCH.sub. 2 CH.sub.3                                                                       H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 S(O).sub.2 -n-C.sub.4 H.sub.9                                                             H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 5h                                     __________________________________________________________________________      ##STR84##                                                                     R.sub.16 R.sub.17                                                                            R.sub.21                                                                          X     Y            m.p. (° C.)                         __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                       H    H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                    Cl       H    H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                              Cl       H    H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                      H        H    H  OCH.sub.3                                                                            CH.sub.2 OCONHCH.sub.3                                  CO.sub.2 CH(CH.sub.3).sub.2                                                             5-F  H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                             CO.sub.2 CH(CH.sub.3).sub.2                                                             H    CH.sub.3                                                                          CH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                               NO.sub.2 H    H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                                NO.sub.2 6-Br H  CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                             Cl       4-Cl H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       CF.sub.3 H    H  OCH.sub.3                                                                            CH(OCH(CH.sub.3)CH.sub.2)                               Cl       6-CH.sub.3                                                                          H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                      C.sub.2 H.sub.5                                                                         H    H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OCOCH.sub.3                                    CH(CH.sub.3).sub.2                                                                      H    H  CH.sub.3                                                                             CH.sub.2 OCON(CH.sub.3).sub.2                           SO.sub.2 CH.sub.3                                                                       H    H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 CH.sub.3                                                                       4-OCH.sub.3                                                                         H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                    SO.sub.2 CH.sub.3                                                                       6-F  H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                               SO.sub.2 H-n-C.sub.4 H.sub.9                                                                 H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                              SO.sub.2 N(CH.sub.3).sub.2                                                              H    H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OCO.sub.2  -n-C.sub.3 H.sub.7                  SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                       H    H  CH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                           H    H  CH.sub.3                                                                             CH.sub.2 OCON(CH.sub.3)(   .sub.-n-C.sub.3                                     H.sub.7)                                                SO.sub.2 H-n-C.sub.3 H.sub.7                                                                 H  CH.sub.3                                                                             CH.sub.2 OCO .sub.-i-C.sub.3 H.sub.7                    SO.sub.2 H.sub.-i-C.sub.3 H.sub.7                                                            H  OCH.sub.3                                                                            CH.sub.2 OCONH(  -n-C.sub.3 H.sub.7)                    SCH.sub.3                                                                               H    H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                              S(O).sub.2 CH.sub.3                                                                     H    H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                              SCH.sub.2 CH.sub.3                                                                      H    CH.sub.3                                                                          OCH.sub.3                                                                            CH.sub.2 OCO.sub.2  .sub.-i-C.sub.3 H.sub.7             S(O).sub.2  -n-C.sub.4 H.sub.9                                                          H    H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                      SO.sub.2 CH.sub.2 CH.sub.3                                                              H    H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                     Cl       H    H  OCH.sub.3                                                                            C(C.sub.2 H.sub.5)(OCH.sub.2 CH.sub.2 O)                NO.sub.2 H    H  OCH.sub.3                                                                            C(CH.sub.3)(SCH.sub.3).sub.2                            NO.sub.2 H    H  OCH.sub.3                                                                            CH.sub.2 S(O)CH.sub.3                                   __________________________________________________________________________

                                      TABLE 6a                                     __________________________________________________________________________      ##STR85##                                                                     R.sub.16 R.sub.17                                                                           R.sub.21                                                                          X     Y         m.p. (° C.)                             __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                       H   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      Cl       H   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      CO.sub.2 CH.sub.3                                                                       H   H  Cl    CH(OCH.sub.3).sub.2                                      Cl       H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      H        H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      CO.sub.2 CH(CH.sub.3).sub.2                                                             5-F H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      CO.sub.2 CH(CH.sub.3).sub.2                                                             H   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      NO.sub.2 H   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      NO.sub.2 6-Br                                                                               H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      CF.sub.3 H   H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                      Cl       6-CH.sub.3                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      C.sub.2 H.sub.5                                                                         H   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      CH(CH.sub.3).sub.2                                                                      H   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      SO.sub.2 CH.sub.3                                                                       H   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      SO.sub.2 CH.sub.3                                                                       6-F H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      SO.sub.2 H-n-C.sub.4 H.sub.9                                                                CH.sub.3                                                                          CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      SO.sub.2 N(CH.sub.3).sub.2                                                              H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                       H   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                           H   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      SO.sub.2 H-n-C.sub.3 H.sub.7                                                                H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      SO.sub.2 H.sub.-i-C.sub.3 H.sub.7                                                           H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      SCH.sub.3                                                                               H   H  CH.sub.3                                                                             CH(OCH.sub.3 ).sub.2                                     S(O).sub.2 CH.sub.3                                                                     H   H  CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                      SCH.sub.2 CH.sub.3                                                                      H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      S(O).sub.2 (CH.sub.2).sub.3 CH.sub.3                                                    H   H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      CH.sub.3 H   H  CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                             CO.sub.2 CH.sub.2 CH.sub.3                                                              H   H  CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                             SCH.sub.3                                                                               H   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                             Cl       H   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                             __________________________________________________________________________

                                      TABLE 6b                                     __________________________________________________________________________      ##STR86##                                                                     R.sub.16  R.sub.17                                                                             R.sub.21                                                                           X     Y     m.p. (° C.)                             __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                             CH.sub.2 OTHP                                        Cl        H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OTHP                                        Cl        H     H   OCH.sub.3                                                                            CH.sub.2 OTHP                                        H         H     H   OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OTHP                                        CO.sub.2 CH(CH.sub.3).sub.2                                                              5-F   H   CH.sub.3                                                                             CH.sub.2 OTHP                                        CO.sub.2 CH(CH.sub.3).sub.2                                                              H     H   CH.sub.3                                                                             CH.sub.2 OTHP                                        NO.sub.2  H     H   CH.sub.3                                                                             CH.sub.2 OTHP                                        NO.sub.2  6-Br  H   CH.sub.3                                                                             CH.sub.2 OTHP                                        Cl        2-Cl  H   OCH.sub.3                                                                            CH.sub.2 OTHP                                        CF.sub.3  H     H   OCH.sub.3                                                                            CH.sub.2 OTHP                                        Cl        6-CH.sub.3                                                                           H   OCH.sub.3                                                                            CH.sub.2 OTHP                                        C.sub.2 H.sub.5                                                                          H     H   CH.sub.2 CH.sub.3                                                                    CH.sub.2 OTHP                                        CH(CH.sub.3).sub.2                                                                       H     H   CH.sub.3                                                                             CH.sub.2 OTHP                                        SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                             CH.sub.2 OTHP                                        SO.sub.2 CH.sub.3                                                                        5-OCH.sub.3                                                                          H   OCH.sub.3                                                                            CH.sub.2 OTHP                                        SO.sub.2 CH.sub.3                                                                        6-F   H   OCH.sub.3                                                                            CH.sub.2 OTHP                                        SO.sub.2  -n-C.sub.4 H.sub.9                                                             H     H   CH.sub.3                                                                             CH.sub.2 OTHP                                        SO.sub.2 N(CH.sub.3).sub.2                                                               H     CH.sub.3                                                                           OCH.sub.3                                                                            CH.sub.2 OTHP                                        SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                        H     CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OTHP                                        SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H     H   CH.sub.3                                                                             CH.sub.2 OTHP                                        SO.sub.2  -n-C.sub.3 H.sub.7                                                             H     H   CH.sub.3                                                                             CH.sub.2 OTHP                                        SO.sub.2  .sub.-i-C.sub.3 H.sub.7                                                        H     H   OCH.sub.3                                                                            CH.sub.2 OTHP                                        SCH.sub.3 H     H   CH.sub.3                                                                             CH.sub.2 OTHP                                        S(O).sub.2 CH.sub. 3                                                                     H     H   CH.sub.3                                                                             CH.sub.2 OTHP                                        SCH.sub.2 CH.sub.3                                                                       H     H   OCH.sub.3                                                                            CH.sub.2 OTHP                                        S(O).sub.2  -n-C.sub.4 H.sub.9                                                           H     H   OCH.sub.3                                                                            CH.sub.2 OTHP                                        __________________________________________________________________________

                  TABLE 6c                                                         ______________________________________                                          ##STR87##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                               X       Y     (° C.)                        ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H       CH.sub.3                                                                               CH.sub.2 OH                                Cl         H        H       CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                Cl         H        H       OCH.sub.3                                                                              CH.sub.2 OH                                H          H        H       OCH.sub.3                                                                              CH.sub.2 OH                                CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H       CH.sub.3                                                                               CH.sub.2 OH                                CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H       CH.sub.3                                                                               CH.sub.2 OH                                NO.sub.2   H        H       CH.sub.3                                                                               CH.sub.2 OH                                NO.sub.2   6-Br     H       CH.sub.3                                                                               CH.sub.2 OH                                Cl         2-Cl     H       OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                CF.sub.3   H        H       OCH.sub.3                                                                              CH.sub.2 OH                                Cl         6-CH.sub.3                                                                              H       OCH.sub.3                                                                              CH.sub.2 OH                                C.sub.2 H.sub.5                                                                           H        H       CH.sub.3                                                                               CH.sub.2 OH                                CH(CH.sub.3).sub.2                                                                        H        H       CH.sub.3                                                                               CH.sub.2 OH                                SO.sub.2 CH.sub.3                                                                         H        H       CH.sub.3                                                                               CH.sub.2 OH                                SO.sub.2 CH.sub.3                                                                         5-OCH.sub.3                                                                             H       OCH.sub.3                                                                              CH.sub.2 OH                                SO.sub.2 CH.sub.3                                                                         6-F      H       OCH.sub.3                                                                              CH.sub.2 OH                                SO.sub.2  -n-C.sub.4 H.sub.9                                                              H        H       CH.sub.3                                                                               CH.sub.2 OH                                SO.sub.2 N(CH.sub.3).sub.2                                                                H        H       OCH.sub.3                                                                              CH.sub.2 OH                                SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H       CH.sub.3                                                                               CH.sub.2 OH                                SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H       CH.sub.3                                                                               CH.sub.2 OH                                SO.sub.2  -n-C.sub.3 H.sub.7                                                              H        H       CH.sub.3                                                                               CH.sub.2 OH                                SO.sub.2  .sub.-i-C.sub.3 H.sub.7                                                         H        CH.sub.3                                                                               OCH.sub.3                                                                              CH.sub.2 OH                                SCH.sub.3  H        CH.sub.3                                                                               CH.sub.3                                                                               CH.sub.2 OH                                S(O).sub.2 CH.sub.3                                                                       H        H       CH.sub.3                                                                               CH.sub.2 OH                                SCH.sub.2 CH.sub.3                                                                        H        H       OCH.sub.3                                                                              CH.sub.2 OH                                S(O).sub.2 H-n-C.sub.4 H.sub.9                                                                     H       OCH.sub.3                                                                              CH.sub.2 OH                                ______________________________________                                    

                                      TABLE 6d                                     __________________________________________________________________________      ##STR88##                                                                     R.sub.16 R.sub.17                                                                            R.sub.21                                                                          X     Y         m.p. (° C.)                            __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                       H    H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                    Cl       H    H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                              Cl       H    H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                      H        H    H  OCH.sub.3                                                                            CH.sub.2 OCONHCH.sub.3                                  CO.sub.2 CH(CH.sub.3).sub.2                                                             5-F  H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                             CO.sub.2 CH(CH.sub.3).sub.2                                                             H    H  CH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                               NO.sub.2 H    H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                                NO.sub.2 6-Br H  CH.sub.3                                                                             CH.sub.2 OCOC.sub. 2 H.sub.5                            Cl       2-Cl H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       CF.sub.3 H    H  OCH.sub.3                                                                            CH(OCH(CH.sub.3)CH.sub.2)                               Cl       6-CH.sub.3                                                                          CH.sub.3                                                                          OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                      C.sub.2 H.sub.5                                                                         H    CH.sub.3                                                                          CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                    CH(CH.sub.3).sub.2                                                                      H    H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OCON(CH.sub.3).sub.2                           SO.sub.2 CH.sub.3                                                                       H    H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                                SO.sub.2 CH.sub.3                                                                       5-OCH.sub.3                                                                         H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                    SO.sub.2 CH.sub.3                                                                       6-F  H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                               SO.sub.2 H-n-C.sub.4 H.sub.9                                                                 H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                              SO.sub.2 N(CH.sub.3).sub.2                                                              H    H  OCH.sub.3                                                                            CH.sub.2 OCO.sub.2  -n-C.sub.3 H.sub.7                  SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                       H    H  CH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                           H    H  CH.sub.3                                                                             CH.sub.2 OCON(CH.sub.3)( - n-C.sub.3 H.sub.7)           SO.sub.2 H-n-C.sub.3 H.sub.7                                                                 H  CH.sub.3                                                                             CH.sub.2 OCO .sub.-i-C.sub.3 H.sub.7                    SO.sub.2 H.sub.-i-C.sub.3 H.sub.7                                                            H  OCH.sub.3                                                                            CH.sub.2 OCONH( -n-C.sub.3 H.sub.7) -                                          SCH.sub.3 H H CH.sub.3 CH(OC.sub.2 H.sub.5).sub.2       S(O).sub.2 CH.sub.3                                                                     H    H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                              SCH.sub.2 CH.sub.3                                                                      H    H  OCH.sub.3                                                                            CH.sub.2 OCO.sub.2  .sub.-i-C.sub.3 H.sub.7             S(O).sub.2 -n-C.sub.4 H.sub.9                                                           H    H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 SCH.sub.3                                      CH.sub.3 H    H  OCH.sub.3                                                                            CH(SCH.sub.2 CH.sub.3).sub.2                            NO.sub.2 H    H  OCH.sub.3                                                                            CH(SCH.sub.3).sub.2                                     SO.sub.2 N(CH.sub.3).sub.2                                                              H    H  C.sub.2 H.sub.5                                                                      CH.sub.2 SO.sub.2 CH.sub.3                              SO.sub.2 N(CH.sub.3).sub.2                                                              H    H  OCH.sub.3                                                                            CH.sub.2 S(O)CH.sub.3                                   SO.sub.2 N(CH.sub.3).sub.2                                                              H    H  CH.sub. 3                                                                            CH.sub.2 S(O)CH.sub.2 CH.sub.3                          __________________________________________________________________________

                                      TABLE 6e                                     __________________________________________________________________________      ##STR89##                                                                     R.sub.16 R.sub.17                                                                            R.sub.21                                                                          X     Y         m.p. (° C.)                            __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                       H    CH.sub.3                                                                          CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     Cl       H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     Cl       H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     H        H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CO.sub.2 CH(CH.sub.3).sub.2                                                             5-F  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     CO.sub.2 CH(CH.sub.3).sub.2                                                             H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     NO.sub.2 H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     NO.sub.2 6-Br H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     CF.sub.3 H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     Cl       6-CH.sub.3                                                                          H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     C.sub.2 H.sub.5                                                                         H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     CH(CH.sub.3).sub.2                                                                      H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                       H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                       5-OCH.sub.3                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 CH.sub.3                                                                       6-F  H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 H-n-C.sub.4 H.sub.9                                                                 H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 N(CH.sub.3).sub.2                                                              H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                       H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 N(OCH.sub.3)CH.sub.3                                                           H    CH.sub.3                                                                          CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                     SO.sub.2 H-n-C.sub.3 H.sub.7                                                                 H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SO.sub.2 H.sub.-i-C.sub.3 H.sub.7                                                            H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                     SCH.sub.3                                                                               H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     S(O).sub.2 CH.sub.3                                                                     H    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     SCH.sub.2 CH.sub.3                                                                      H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     S(O).sub.2 (CH.sub.2).sub.3 CH.sub.3                                                    H    H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     CH(CH.sub.3).sub.2                                                                      H    H  OCH.sub.3                                                                            C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2                   CO.sub.2 CH(CH.sub.3).sub.2                                                             H    H  OCH.sub.3                                                                            C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2                   CF.sub.3 H    H  OCH.sub.3                                                                            C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2                   __________________________________________________________________________

                  TABLE 6f                                                         ______________________________________                                          ##STR90##                                                                                                             m.p.                                   R.sub.16   R.sub.17 R.sub.21X   Y       (°C.)                           ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        HCH.sub.3   CH.sub.2 OTHP                                  Cl         H        HCH.sub.3   CH.sub.2 OTHP                                  Cl         H        HOCH.sub.3  CH.sub.2 OTHP                                  H          H        HOCH.sub.3  CH.sub.2 OTHP                                  CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      CH.sub.3CH.sub.3                                                                           CH.sub.2 OTHP                                  CO.sub.2 CH(CH.sub.3).sub.2                                                               H        CH.sub.3CH.sub.3                                                                           CH.sub.2 OTHP                                  NO.sub.2   H        HCH.sub.3   CH.sub.2 OTHP                                  NO.sub.2   6-Br     H CH.sub.3  CH.sub.2 OTHP                                  Cl         2-Cl     HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OTHP                                  CF.sub.3   H        HOCH.sub.3  CH.sub.2 OTHP                                  Cl         6-CH.sub.3                                                                              HOCH.sub.3  CH.sub.2 OTHP                                  C.sub.2 H.sub.5                                                                           H        HCH.sub.3   CH.sub.2 OTHP                                  CH(CH.sub.3).sub.2                                                                        H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         5-OCH.sub.3                                                                             HOCH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 CH.sub.3                                                                         6-F      HOCH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 N(CH.sub.3).sub.2                                                                H        HOCH.sub.3  CH.sub.2 OTHP                                  SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        HCH.sub.2 CH.sub.3                                                                         CH.sub.2 OTHP                                  SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        HCH.sub.3   CH.sub.2 OTHP                                  SO.sub.2 .sub.- i-C.sub.3 H.sub.7                                                         H        HOCH.sub.3  CH.sub.2 OTHP                                  SCH.sub.3  H        HCH.sub.3   CH.sub.2 OTHP                                  S(O).sub.2 CH.sub.3                                                                       H        HCH.sub.3   CH.sub.2 OTHP                                  SCH.sub.2 CH.sub.3                                                                        H        HOCH.sub.3  CH.sub.2 OTHP                                  S(O).sub.2 -n-C.sub.4 H.sub.9                                                             H        HOCH.sub.3  CH.sub.2 OTHP                                  ______________________________________                                    

                  TABLE 6g                                                         ______________________________________                                          ##STR91##                                                                                                               m.p.                                 R.sub.16   R.sub.17 R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         CO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 H          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               5-F      H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OH                                 CO.sub.2 CH(CH.sub.3).sub.2                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   H        H      CH.sub.3                                                                               CH.sub.2 OH                                 NO.sub.2   6-Br     H      CH.sub.3                                                                               CH.sub.2 OH                                 Cl         2-Cl     H      OCH.sub.3                                                                              CH.sub.2 OH                                 CF.sub.3   H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 Cl         6-CH.sub.3                                                                              H      OCH.sub.3                                                                              CH.sub.2 OH                                 C.sub.2 H.sub.5                                                                           H        H      CH.sub.3                                                                               CH.sub.2 OH                                 CH(CH.sub.3).sub.2                                                                        H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         5-OCH.sub.3                                                                             H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 CH.sub.3                                                                         6-F      H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 -n-C.sub.4 H.sub.9                                                               H        CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(CH.sub.3).sub.2                                                                H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                         H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 -n-C.sub.3 H.sub.7                                                               H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          H        H      OCH.sub.3                                                                              CH.sub.2 OH                                 SCH.sub.3  H        H      CH.sub.3                                                                               CH.sub.2 OH                                 S(O).sub.2 CH.sub.3                                                                       H        H      CH.sub.3                                                                               CH.sub.2 OH                                 SCH.sub.2 CH.sub.3                                                                        H        H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                 S(O).sub.2 H-n-C.sub.4 H.sub.9                                                                     H      OCH.sub.3                                                                              CH.sub.2 OH                                 ______________________________________                                    

                                      TABLE 6h                                     __________________________________________________________________________      ##STR92##                                                                     R.sub.16  R.sub.17                                                                             R.sub.21                                                                           X      Y            m.p. (°C.)                      __________________________________________________________________________     CO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                                Cl        H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          Cl        H     H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  H         H     H   OCH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                              CO.sub.2 CH(CH.sub.3).sub.2                                                              5-F   H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                         CO.sub.2 CH(CH.sub.3).sub.2                                                              H     H   CH.sub.3                                                                              CH.sub.2 SC.sub.2 H.sub.5                           NO.sub.2  H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            NO.sub.2  6-Br  H   CH.sub.3                                                                              CH.sub.2 OCOC.sub.2 H.sub.5                         Cl        2-Cl  H   OCH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                   CF.sub.3  H     H   OCH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2)                           Cl        6-CH.sub.3                                                                           H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  C.sub.2 H.sub.5                                                                          H     H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                                CH(CH.sub.3).sub.2                                                                       H     CH.sub.3                                                                           CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3).sub.2                       SO.sub.2 CH.sub.3                                                                        H     H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                            SO.sub.2 CH.sub.3                                                                        5-OCH.sub.3                                                                          H   OCH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                SO.sub.2 CH.sub.3                                                                        6-F   H   OCH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                           SO.sub.2 -n-C.sub.4 H.sub.9                                                              H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SO.sub.2 N(CH.sub.3).sub.2                                                               H     H   OCH.sub.2 CH.sub.3                                                                    CH.sub.2 OCO.sub.2 -n-C.sub.3 H.sub.7               SO.sub.2 N(C.sub.2 H.sub.5).sub.2                                                        H     H   CH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H     H   CH.sub.3                                                                              CH.sub.2 OCON(CH.sub.3)( -n-C.sub.3 H.sub.7)        SO.sub.2 -n-C.sub.3 H.sub.7                                                              H     H   CH.sub.3                                                                              CH.sub.2 OCO .sub.-i-C.sub.3 H.sub.7                SO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                         H     H   OCH.sub.3                                                                             CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)                 SCH.sub.3 H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          S(O).sub.2 CH.sub.3                                                                      H     H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                          SCH.sub.2 CH.sub.3                                                                       H     H   OCH.sub.2 CH.sub.3                                                                    CH.sub.2 OCO.sub.2 .sub.-i-C.sub.3 H.sub.7          S(O).sub.2 -n-C.sub.4 H.sub.9                                                            H     CH.sub.3                                                                           OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                  SCH.sub.2 CH.sub.3                                                                       H     H   OC.sub.2 H.sub.5                                                                      C(CH.sub.3)(OCH.sub.2 CH.sub.2 CH.sub.2 O)          Cl        H     H   CH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                          CH.sub.3  H     H   OCH.sub.3                                                                             CH(SCH.sub.2 CH.sub.3).sub.2                        __________________________________________________________________________

                                      TABLE 7a                                     __________________________________________________________________________      ##STR93##                                                                     R.sub.17                                                                             R.sub.18    R.sub.21                                                                           X      Y          m.p. (°C.)                      __________________________________________________________________________     H     CO.sub.2 CH.sub.3                                                                          H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               4-CH.sub.3                                                                           CO.sub.2 CH.sub.3                                                                          H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     CO.sub.2 CH.sub.3                                                                          H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     H           H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     SCH.sub.2 CH.sub.2 CH.sub.3                                                                H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     SCH.sub.3   H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     CH(CH.sub.3).sub.2                                                                         H   OCH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                               H     CH.sub.2 CH.sub.3                                                                          H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     F           H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     Cl          H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               5-Cl  Cl          H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     Br          CH.sub.3                                                                           OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     NO.sub.2    H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                      H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     SO.sub.2 N(CH.sub.3).sub.2                                                                 H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     SO.sub.2 N(OCH.sub.3)CH.sub.3                                                              H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     OCH.sub.3   CH.sub.3                                                                           CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               5-OCH.sub.3                                                                          OCH.sub.3   H   CH.sub.2 CH.sub.3                                                                     CH(OCH.sub.3).sub.2                               5-F   O(CH.sub.2).sub.3 CH.sub.3                                                                 H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H   OCH.sub.3                                                                             CH(OCH.sub.3).sub.2                               H     SO.sub.2 CH.sub.3                                                                          H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               4-Br  SO.sub.2 CH.sub.3                                                                          H   CH.sub.3                                                                              CH(OCH.sub.3).sub.2                               H     CO.sub.2 CH.sub.3                                                                          H   Cl     CH(OCH.sub.3).sub.2                               H     NO.sub.2    H   Cl     CH(OCH.sub.3).sub.2                               H     Cl          H   OCH.sub. 3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                      H     CO.sub.2 CH.sub.3                                                                          H   OCH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                      H     CO.sub.2 CH.sub.3                                                                          H   OCH.sub.3                                                                             C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2             H     SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H   Cl     CH(OCH.sub.3).sub.2                               H     SO.sub.2 CH.sub.3                                                                          H   Cl     CH(OCH.sub.3).sub.2                               H     SCH.sub.3   H   Cl     CH(OCH.sub.3).sub.2                               __________________________________________________________________________

                  TABLE 7b                                                         ______________________________________                                          ##STR94##                                                                                                               m.p.                                 R.sub.17                                                                             R.sub.18      R.sub.21                                                                              X       Y      (°C.)                         ______________________________________                                         H     CO.sub.2 CH.sub.3                                                                            H      CH.sub.3                                                                               CH.sub.2 OTHP                               4-CH.sub.3                                                                           CO.sub.2 CH.sub.3                                                                            H      CH.sub.2 CH.sub.3                                                                      CH.sub.2 OTHP                               H     CO.sub.2 CH.sub.2 CH.sub.3                                                                   H      OCH.sub.3                                                                              CH.sub.2 OTHP                               H     CO.sub.2 CH.sub.2 CHCH.sub.2                                                                 H      CH.sub.3                                                                               CH.sub.2 OTHP                               H     H             H      CH.sub.3                                                                               CH.sub.2 OTHP                               H     SCH.sub.2 CH.sub.2 CH.sub.3                                                                  H      OCH.sub.3                                                                              CH.sub.2 OTHP                               H     SCH.sub.3     H      CH.sub.3                                                                               CH.sub.2 OTHP                               H     CH(CH.sub.3).sub.2                                                                           H      OCH.sub.3                                                                              CH.sub.2 OTHP                               H     CH.sub.2 CH.sub.3                                                                            H      CH.sub.3                                                                               CH.sub.2 OTHP                               H     F             H      OCH.sub.3                                                                              CH.sub.2 OTHP                               H     Cl            H      OCH.sub.3                                                                              CH.sub.2 OTHP                               5-Cl  Cl            H      CH.sub.3                                                                               CH.sub.2 OTHP                               H     Br            CH.sub.3                                                                              OCH.sub.3                                                                              CH.sub.2 OTHP                               H     NO.sub.2      CH.sub.3                                                                              CH.sub.3                                                                               CH.sub.2 OTHP                               H     SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                        H      CH.sub.3                                                                               CH.sub.2 OTHP                               H     SO.sub.2 N(CH.sub.3).sub.2                                                                   H      OCH.sub.3                                                                              CH.sub.2 OTHP                               H     SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                H      OCH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                               H     OCH.sub.3     H      CH.sub.3                                                                               CH.sub.2 OTHP                               5-    OCH.sub.3     H      CH.sub.3                                                                               CH.sub.2 OTHP                               OCH.sub.3                                                                      5-F   O(CH.sub.2).sub.3 CH.sub.3                                                                   H      OCH.sub.3                                                                              CH.sub.2 OTHP                               H     SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                          H      OCH.sub.3                                                                              CH.sub.2 OTHP                               H     SO.sub.2 CH.sub.3                                                                            H      CH.sub.3                                                                               CH.sub.2 OTHP                               4-Br  SO.sub.2 CH.sub.3                                                                            H      CH.sub.3                                                                               CH.sub.2 OTHP                               ______________________________________                                    

                  TABLE 7c                                                         ______________________________________                                          ##STR95##                                                                                                           m.p.                                     R.sub.17R.sub.18 R.sub.21X   Y        (°C.)                             ______________________________________                                         HCO.sub.2 CH.sub.3                                                                              HCH.sub.3   CH.sub.2 OH                                                                             143-                                                                           147°                              4-CH.sub.3CO.sub.2 CH.sub.3                                                                     HCH.sub.3   CH.sub.2 OH                                       HCO.sub.2 CH.sub.2 CH.sub.3                                                                     HOCH.sub.3  CH.sub.2 OH                                       HCO.sub.2 CH.sub.2 CHCH.sub.2                                                                   HCH.sub.3   CH.sub.2 OH                                       HH               HCH.sub.3   CH.sub.2 OH                                       HSCH.sub.2 CH.sub.2 CH.sub.3                                                                    HOCH.sub.3  CH.sub.2 OH                                       H SCH.sub.3      HCH.sub.3   CH.sub.2 OH                                       HCH(CH.sub.3).sub.2                                                                             HOCH.sub.3  CH.sub.2 OH                                       HCH.sub.2 CH.sub.3                                                                              CH.sub.3CH.sub.3                                                                           CH.sub.2 OH                                       HF               HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OH                                       HCl              CH.sub.3OCH.sub.3                                                                          CH.sub.2 OH                                       5-ClCl           HCH.sub.2 CH.sub.3                                                                         CH.sub.2 OH                                       HBr              HOCH.sub.3  CH.sub.2 OH                                       HNO.sub.2        HCH.sub.3   CH.sub.2 OH                                       HSO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                          HCH.sub.3   CH.sub.2 OH                                       HSO.sub.2 N(CH.sub.3).sub.2                                                                     HOCH.sub.3  CH.sub.2 OH                                       HSO.sub.2 N(OCH.sub.3)CH.sub.3                                                                  HOCH.sub.3  CH.sub.2 OH                                       HOCH.sub.3       HCH.sub.3   CH.sub.2 OH                                       5-OCH.sub.3OCH.sub.3                                                                            HCH.sub.3   CH.sub.2 OH                                       5-FO(CH.sub.2).sub.3 CH.sub.3                                                                   HOCH.sub. 3 CH.sub.2 OH                                       HSO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                            HOCH.sub.3  CH.sub.2 OH                                       HSO.sub.2 CH.sub.3                                                                              HCH.sub.3   CH.sub.2 OH                                       4-BrSO.sub.2 CH.sub.3                                                                           HCH.sub.3   CH.sub.2 OH                                       ______________________________________                                    

                                      TABLE 7d                                     __________________________________________________________________________      ##STR96##                                                                     R.sub.17                                                                             R.sub.18   R.sub.21                                                                           X      Y           m.p. (°C.)                      __________________________________________________________________________     H     CO.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                         4-CH.sub.3                                                                           CO.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                               H     CO.sub.2 CH.sub.3                                                                         H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                 H     CO.sub.2 CH.sub.2 CHCH.sub.2                                                              H   CH.sub.3                                                                              CH.sub.2 OCONHCH.sub.3                             H     H          H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 CH.sub.3                        H     SCH.sub.2 CH.sub.2 CH.sub.3                                                               H   OCH.sub.3                                                                             CH.sub.2 SC.sub.2 H.sub.5                          H     SCH.sub.3  H   CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                           H     CH(CH.sub.3).sub.2                                                                        H   OCH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                        H     CH.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                              CH(OCH(CH.sub.3)CH.sub.2 O)                        H     F          H   OCH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                  H     Cl         H   OCH.sub.3                                                                             CH.sub.2 SCH.sub.3                                 5-Cl  Cl         H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                               H     Br         CH.sub.3                                                                           OCH.sub.3                                                                             CH.sub.2 OCON(CH.sub.3).sub.2                      H     NO.sub.2   CH.sub.3                                                                           CH.sub.3                                                                              CH(OCH.sub.2 CH.sub.2 O)                           H     SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                       H   CH.sub.3                                                                              CH.sub.2 OCOCH.sub.3                               H     SO.sub.2 N(CH.sub.3).sub.2                                                                H   OCH.sub.2 CH.sub.3                                                                    CH.sub.2 SCH.sub.2 CH.sub.3                        H     SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H   CH.sub.3                                                                              CH(OC.sub.2 H.sub.5).sub.2                         H     OCH.sub.3  H   CH.sub.3                                                                              CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                 5-OCH.sub.3                                                                          OCH.sub.3  H   CH.sub.3                                                                              CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2               5-F   O(CH.sub.2).sub.3 CH.sub.3                                                                H   OCH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2               H     SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                       H   CH.sub.3                                                                              CH.sub.2 OCO( .sub.-i-C.sub.3 H.sub.7)             H     SO.sub.2 CH.sub.3                                                                         H   CH.sub.2 CH.sub.3                                                                     CH.sub.2 OCONH(  -n-C.sub.3 H.sub.7)               H     SCH.sub.3  H   CH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                         H     CH.sub.3   H   CH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                H     CO.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                              CH.sub.2 SO.sub.2 CH.sub.3                         __________________________________________________________________________

                                      TABLE 7e                                     __________________________________________________________________________      ##STR97##                                                                     R.sub.17                                                                            R.sub.18   R.sub.21                                                                          X     Y        m.p. (°C                              __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   4-CH.sub.3                                                                          CO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.3                                                                         H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                              H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    H          CH.sub.3                                                                          CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SCH.sub.2 CH.sub.2 CH.sub.3                                                               H  OCH.sub.3                                                                            CH(OCH.sub. 3).sub.2                                  H    SCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CH(CH.sub.3).sub.2                                                                        H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    CH.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    F          H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    Cl         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   5-Cl Cl         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    Br         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    NO.sub.2   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                     H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(CH.sub.3).sub.2                                                                CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    OCH.sub.3  H  CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                   5-OCH.sub.3                                                                         OCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub. 3).sub.2                                  5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                       H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   4-Br SO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    Cl         H  CH.sub.3                                                                             C(CH.sub. 3)(OCH.sub. 3).sub.2                        H    Br         H  OCH.sub.3                                                                            C(CH.sub. 3)(OCH.sub. 3).sub.2                        H    SO.sub.2 CH.sub.3                                                                         H  OCH.sub.3                                                                            C(CH.sub. 3)(OCH.sub. 3).sub.2                        H    CO.sub.2 CH.sub.3                                                                         H  OCH.sub.3                                                                            C(CH.sub. 3)(OCH.sub. 3).sub.2                        __________________________________________________________________________

                                      TABLE 7f                                     __________________________________________________________________________      ##STR98##                                                                     R.sub.17                                                                            R.sub.18    R.sub.21                                                                          X      Y     m.p. (°C.)                             __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       4-CH.sub.3                                                                          CO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    CO.sub.2 CH.sub.2 CH.sub.3                                                                 H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H  CH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                       H    H           H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    SCH.sub.2 CH.sub.2 CH.sub.3                                                                H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    SCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    CH(CH.sub.3).sub.2                                                                         H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    CH.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    F           H  OCH.sub.2 CH.sub.3                                                                    CH.sub.2 OTHP                                       H    Cl          H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       5-Cl Cl          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    Br          CH.sub.3                                                                          OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    NO.sub.2    H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                      CH.sub.3                                                                          CH.sub.3                                                                              CH.sub.2 OTHP                                       H    SO.sub.2 N(CH.sub.3).sub.2                                                                 H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                              H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    OCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OTHP                                       5-OCH.sub.3                                                                         OCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OTHP                                       5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                 H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    SO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       4-Br SO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       __________________________________________________________________________

                                      TABLE 7g                                     __________________________________________________________________________      ##STR99##                                                                     R.sub.17                                                                            R.sub.18    R.sub.21                                                                          X      Y     m.p. (°C.)                             __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OH                                         4-CH.sub.3                                                                          CO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OH                                         H    CO.sub.2 CH.sub.2 CH.sub.3                                                                 CH.sub.3                                                                          OCH.sub.3                                                                             CH.sub.2 OH                                         H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H  CH.sub.3                                                                              CH.sub.2 OH                                         H    H           H  CH.sub.3                                                                              CH.sub.2 OH                                         H    SCH.sub.2 CH.sub.2 CH.sub.3                                                                H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    SCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OH                                         H    CH(CH.sub.3).sub.2                                                                         H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    CH.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OH                                         H    F           H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    Cl          H  OCH.sub.2 CH.sub.3                                                                    CH.sub.2 OH                                         5-Cl Cl          H  CH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                         H    Br          H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    NO.sub.2    H  CH.sub.3                                                                              CH.sub.2 OH                                         H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                      H  CH.sub.3                                                                              CH.sub.2 OH                                         H    SO.sub.2 N(CH.sub.3).sub.2                                                                 H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                              H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    OCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OH                                         5-OCH.sub.3                                                                         OCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OH                                         5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                 H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    SO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OH                                         4-Br SO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OH                                         __________________________________________________________________________

                                      TABLE 7h                                     __________________________________________________________________________      ##STR100##                                                                    R.sub.17                                                                            R.sub.18  R.sub.21                                                                          X     Y            m.p. (°C.)                         __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             4-CH.sub.3                                                                          CO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                   H    CO.sub.2 CH.sub.3                                                                        H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H  CH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                                 H    H         H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                            H    SCH.sub.2 CH.sub.2 CH.sub.3                                                              H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                              H    SCH.sub.3 H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                               H    CH(CH.sub.3).sub.2                                                                       H  OCH.sub.3                                                                            CH.sub.2 OCOC.sub.2 H.sub.5                            H    CH.sub.2 CH.sub.3                                                                        CH.sub.3                                                                          CH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2 O)                            H    F         H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      H    Cl        H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     5-Cl Cl        H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OCOCH.sub.3                                   H    Br        H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OCON(CH.sub.3).sub.2                          H    NO.sub.2  H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                               H    SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                      H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                   H    SO.sub.2 N(CH.sub.3).sub.2                                                               H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.2 CH.sub.3                            H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             H    OCH.sub.3 H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                     5-OCH.sub.3                                                                         OCH.sub.3 H  CH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                   5-F  O(CH.sub.2).sub.3 CH.sub.3                                                               H  OCH.sub.3                                                                            CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                   H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                      H  CH.sub.3                                                                             CH.sub.2 OCO( .sub.-i-C.sub.3 H.sub.7)                 H    SO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH.sub. 2 OCONH( -n-C.sub.3 H.sub.7)                   H    CO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.2 CH.sub.2 CH.sub.2 O)             H    CO.sub.2 CH.sub.3                                                                        H  OCH.sub.3                                                                            C(CH.sub.3)(SCH.sub.3).sub.2                           H    CO.sub.2 CH.sub.3                                                                        H  OCH.sub.3                                                                            CH(SCH.sub.3).sub.2                                    H    Cl        H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                    __________________________________________________________________________

                                      TABLE 8a                                     __________________________________________________________________________      ##STR101##                                                                    R.sub.17                                                                            R.sub.18   R.sub.21                                                                          X     Y        m.p. (°C.)                            __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   4-CH.sub.3                                                                          CO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.3                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                              H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    H          H  CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                   H    SCH.sub.2 CH.sub.2 CH.sub.3                                                               H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                   H    SCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CH(CH.sub.3).sub.2                                                                        H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    CH.sub.2 CH.sub. 3                                                                        H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    F          H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    Cl         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   5-Cl Cl         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    Br         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    NO.sub.2   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                     H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(CH.sub.3).sub.2                                                                H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    OCH.sub.3  CH.sub.3                                                                          CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   5-OCH.sub.3                                                                         OCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                       H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   4-Br SO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.3                                                                         H  Cl    CH(OCH.sub.3 .sub.2                                   H    NO.sub.2   H  Cl    CH(OCH.sub.3).sub.2                                   H    CH.sub.3   H  CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                          H    CH.sub.3   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                          H    SCH.sub.3  H  CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                          H    Br         H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                          H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                       H  Cl    CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.3                                                                         H  Cl    CH(OCH.sub.3).sub.2                                   H    SCH.sub.3  H  Cl    CH(OCH.sub.3).sub.2                                   H    SO.sub.2 -n-C.sub.3 H.sub.7                                                               H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                                                     121-124° d                            __________________________________________________________________________

                                      TABLE 8b                                     __________________________________________________________________________      ##STR102##                                                                    R.sub.17                                                                            R.sub.18    R.sub.21                                                                          X      Y     m.p. (°C.)                             __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       4-CH.sub.3                                                                          CO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    CO.sub.2 CH.sub.2 CH.sub.3                                                                 H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    H           H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    SCH.sub.2 CH.sub.2 CH.sub.3                                                                H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    SCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    CH(CH.sub.3).sub.2                                                                         H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    CH.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    F           H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    Cl          H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       5-Cl Cl          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    Br          H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    NO.sub.2    CH.sub.3                                                                          CH.sub.3                                                                              CH.sub.2 OTHP                                       H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                      H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    SO.sub.2 N(CH.sub.3).sub.2                                                                 H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                              H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    OCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OTHP                                       5-OCH.sub.3                                                                         OCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OTHP                                       5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                 H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H  OCH.sub.2 CH.sub.3                                                                    CH.sub.2 OTHP                                       H    SO.sub.2 CH.sub.3                                                                          H  CH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                       4-Br SO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       __________________________________________________________________________

                                      TABLE 8c                                     __________________________________________________________________________      ##STR103##                                                                    R.sub.17                                                                            R.sub.18    R.sub.21                                                                          X      Y     m.p. (°C.)                             __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OH                                         4-CH.sub.3                                                                          CO.sub.2 CH.sub.3                                                                          H  CH.sub.2 CH.sub.3                                                                     CH.sub.2 OH                                         H    CO.sub.2 CH.sub.2 CH.sub.3                                                                 H  OCH.sub.2 CH.sub.3                                                                    CH.sub.2 OH                                         H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H  CH.sub.3                                                                              CH.sub.2 OH                                         H    H           H  CH.sub.3                                                                              CH.sub.2 OH                                         H    SCH.sub.2 CH.sub.2 CH.sub.3                                                                H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    SCH.sub.3   CH.sub.3                                                                          CH.sub.3                                                                              CH.sub.2 OH                                         H    CH(CH.sub.3).sub.2                                                                         H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    CH.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OH                                         H    F           H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    Cl          H  OCH.sub.3                                                                             CH.sub.2 OH                                         5-Cl Cl          H  CH.sub.3                                                                              CH.sub.2 OH                                         H    Br          H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    NO.sub.2    H  CH.sub.3                                                                              CH.sub.2 OH                                         H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                      H  CH.sub.3                                                                              CH.sub.2 OH                                         H    SO.sub.2 N(CH.sub.3).sub.2                                                                 H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                              H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    OCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OH                                         5-OCH.sub.3                                                                         OCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OH                                         5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                 H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H  OCH.sub.3                                                                             CH.sub.2 OH                                         H    SO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OH                                         4-Br SO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OH                                         __________________________________________________________________________

                                      TABLE 8d                                     __________________________________________________________________________      ##STR104##                                                                    R.sub.17                                                                            R.sub.18  R.sub.21                                                                          X     Y           m.p (°C.)                           __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             4-CH.sub.3                                                                          CO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                   H    CO.sub.2 CH.sub.3                                                                        H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H  CH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                                 H    H         H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                            H    SCH.sub.2 CH.sub.2 CH.sub.3                                                              H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 SC.sub.2 H.sub.5                              H    SCH.sub.3 H  CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.2 CH.sub..sub.2 O)                          H    CH(CH.sub.3).sub.2                                                                       H  OCH.sub.3                                                                            CH.sub.2 OCOC.sub.2 H.sub. 5                           H    CH.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2 O)                            H    F         H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      H    Cl        H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     5-Cl Cl        H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                   H    Br        H  OCH.sub.3                                                                            CH.sub.2 OCON(CH.sub.3).sub.2                          H    NO.sub.2  H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                               H    SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                      H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                   H    SO.sub.2 N(CH.sub.3).sub.2                                                               H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.2 CH.sub.3                            H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             H    OCH.sub.3 CH.sub.3                                                                          CH.sub.3                                                                             CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                     5-OCH.sub.3                                                                         OCH.sub.3 H  CH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                   5-F  O(CH.sub.2).sub.3 CH.sub.3                                                               H  OCH.sub.3                                                                            CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                   H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                      H  CH.sub.3                                                                             CH.sub.2 OCO( .sub.-i-C.sub.3 H.sub.7)                 H    SO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH.sub.2 OCONH( - n-C.sub.3 H.sub.7)                   H    Cl        H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                             H    Br        H  CH.sub.3                                                                             CH(SCH.sub.3).sub.2                                    H    F         H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                    H    SO.sub.2 N(CH.sub.3).sub.2                                                               H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.2 CH.sub.3).sub.2                  __________________________________________________________________________

                                      TABLE 8e                                     __________________________________________________________________________      ##STR105##                                                                    R.sub.17                                                                            R.sub.18   R.sub.21                                                                          X     Y          m.p. (°C.)                          __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   4-CH.sub.3                                                                          CO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.3                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                              H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    H          H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SCH.sub.2 CH.sub.2 CH.sub.3                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CH(CH.sub.3).sub.2                                                                        H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    CH.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    F          H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    Cl         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   5-Cl Cl         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    Br         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    NO.sub.2   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                     H  CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(CH.sub.3).sub.2                                                                H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    OCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   5-OCH.sub.3                                                                         OCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                       H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   4-Br SO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    OCH.sub.3  H  CH.sub.2 CH.sub.3                                                                    C(CH.sub.2 CH.sub.3)(OCH.sub.3).sub.2                 H    SCH.sub.3  H  CH.sub. 3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                          H    CH.sub.2 CH.sub.3                                                                         H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                          H    CH.sub.3   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                          __________________________________________________________________________

                                      TABLE 8f                                     __________________________________________________________________________      ##STR106##                                                                    R.sub.17                                                                            R.sub.18    R.sub.21                                                                          X      Y     m.p. (°C.)                             __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       4-CH.sub.3                                                                          CO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    CO.sub.2 CH.sub.2 CH.sub.3                                                                 H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                               H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    H           H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    SCH.sub.2 CH.sub.2 CH.sub.3                                                                H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    SCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    CH(CH.sub.3).sub.2                                                                         H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    CH.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub. 2 OTHP                                      H    F           H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    Cl          CH.sub.3                                                                          OCH.sub.3                                                                             CH.sub.2 OTHP                                       5-Cl Cl          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    Br          H  OCH.sub.2 CH.sub.3                                                                    CH.sub.2 OTHP                                       H    NO.sub.2    H  CH.sub.2 CH.sub.3                                                                     CH.sub.2 OTHP                                       H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                      H  CH.sub.3                                                                              CH.sub.2 OTHP                                       H    SO.sub.2 N(CH.sub.3).sub.2                                                                 H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                              H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    OCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OTHP                                       5-OCH.sub.3                                                                         OCH.sub.3   H  CH.sub.3                                                                              CH.sub.2 OTHP                                       5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                 H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                        H  OCH.sub.3                                                                             CH.sub.2 OTHP                                       H    SO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       4-Br SO.sub.2 CH.sub.3                                                                          H  CH.sub.3                                                                              CH.sub.2 OTHP                                       __________________________________________________________________________

                  TABLE 8g                                                         ______________________________________                                          ##STR107##                                                                                                      m.p.                                         R.sub.17                                                                              R.sub.18       R.sub.21 X  Y(°C.)                                ______________________________________                                         H      CO.sub.2 CH.sub.3                                                                             HCH.sub.3   CH.sub.2 OH                                  4-CH.sub.3                                                                            CO.sub.2 CH.sub.3                                                                             HCH.sub.2 CH.sub.3                                                                         CH.sub.2 OH                                  H      CO.sub.2 CH.sub.2 CH.sub.3                                                                    HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OH                                  H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  HCH.sub.3   CH.sub.2 OH                                  H      H              HCH.sub.3   CH.sub.2 OH                                  H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                   HOCH.sub.3  CH.sub.2 OH                                  H      SCH.sub.3      HCH.sub.3   CH.sub.2 OH                                  H      CH(CH.sub.3).sub.2                                                                            HOCH.sub.3  CH.sub.2 OH                                  H      CH.sub.2 CH.sub.3                                                                             HCH.sub.3   CH.sub.2 OH                                  H      F              HOCH.sub.3  CH.sub.2 OH                                  H      Cl             HOCH.sub.3  CH.sub.2 OH                                  5-Cl   Cl             HCH.sub.3   CH.sub.2 OH                                  H      Br             HOCH.sub.3  CH.sub.2 OH                                  H      NO.sub.2       HCH.sub.3   CH.sub.2 OH                                  H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                         HCH.sub.3   CH.sub.2 OH                                  H      SO.sub.2 N(CH.sub.3).sub.2                                                                    HOCH.sub.3  CH.sub.2 OH                                  H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                 HOCH.sub.3  CH.sub.2 OH                                  H      OCH.sub.3      HCH.sub.3   CH.sub.2 OH                                  5-OCH.sub.3                                                                           OCH.sub.3      HCH.sub.3   CH.sub.2 OH                                  5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                    HOCH.sub.3  CH.sub.2 OH                                  H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                           CH.sub.3 OCH.sub.3                                                                         CH.sub.2 OH                                  H      SO.sub.2 CH.sub.3                                                                             CH.sub.3 CH.sub.3                                                                          CH.sub.2 OH                                  4-Br   SO.sub.2 CH.sub.3                                                                             HCH.sub.3   CH.sub.2 OH                                  ______________________________________                                    

                                      TABLE 8h                                     __________________________________________________________________________      ##STR108##                                                                    R.sub.17                                                                            R.sub.18  R.sub.21                                                                          X     Y            m.p.(°C.)                          __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             4-CH.sub.3                                                                          CO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                   H    CO.sub.2 CH.sub.3                                                                        CH.sub.3                                                                          OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                             CH.sub.3                                                                          CH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                                 H    H         H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                            H    SCH.sub.2 CH.sub.2 CH.sub.3                                                              H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                              H    SCH.sub.3 H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                               H    CH(CH.sub.3).sub.2                                                                       H  OCH.sub.3                                                                            CH.sub.2 OCOC.sub. 2 H.sub.5                           H    CH.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2 O)                            H    F         H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      H    Cl        H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 SCH.sub.3                                     5-Cl Cl        H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OCOCH.sub.3                                   H    Br        H  OCH.sub.3                                                                            CH.sub.2 OCON(CH.sub.3).sub.2                          H    NO.sub.2  H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                               H    SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                      H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                   H    SO.sub.2 N(CH.sub.3).sub.2                                                               H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.2 CH.sub.3                            H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             H    OCH.sub.3 H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                     5-OCH.sub.3                                                                         OCH.sub.3 H  CH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                   5-F  O(CH.sub.2).sub.3 CH.sub.3                                                               H  OCH.sub.3                                                                            CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                   H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                      H  CH.sub.3                                                                             CH.sub.2 OCO( -i-C.sub.3 H.sub.7)                      H    SO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH.sub. 2 OCONH( -n-C.sub.3 H.sub.7)                   H    Br        H  OCH.sub.3                                                                            C(CH.sub.3)(SCH.sub.3).sub.2                           H    NO.sub.2  H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                             H    SO.sub.2 CH.sub.2 CH.sub.3                                                               H  OCH.sub.3                                                                            CH(CH.sub.3)SCH.sub.3                                  H    CO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             C(CH.sub.2 CH.sub.2)(OCH.sub.2 CH.sub.2 O)             __________________________________________________________________________

                                      TABLE 9a                                     __________________________________________________________________________      ##STR109##                                                                    R.sub.17                                                                            R.sub.18   R.sub.21                                                                          X     Y        m.p.(°C.)                             __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.3                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                              H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    H          H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SCH.sub.2 CH.sub.2 CH.sub.3                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CH(CH.sub.3).sub.2                                                                        H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    CH.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    F          CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    Cl         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   5-Cl Cl         CH.sub.3                                                                          CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    Br         H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                   H    NO.sub.2   H  CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                     H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(CH.sub.3).sub.2                                                                H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    OCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   5-OCH.sub.3                                                                         OCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                       H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.3                                                                         H  Cl    CH(OCH.sub.3).sub.2                                   H    NO.sub.2   H  Cl    CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                       H  Cl    CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.3                                                                         H  Cl    CH(OCH.sub.3).sub.2                                   H    SCH.sub.3  H  Cl    CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.3                                                                         H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                          H    SO.sub.2 CH.sub.3                                                                         H  OC.sub.2 H.sub.5                                                                     C(CH.sub.3)(OCH.sub.3).sub.2                          H    Br         H  CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                          H    F          CH.sub.3                                                                          OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                          __________________________________________________________________________

                  TABLE 9b                                                         ______________________________________                                          ##STR110##                                                                                                 m.p.                                              R.sub.17 R.sub.18                                                                               R.sub.21 X  Y(°C.)                                     ______________________________________                                         HCO.sub.2 CH.sub.3                                                                              HCH.sub.3   CH.sub.2 OTHP                                     HCO.sub.2 CH.sub.2 CH.sub.3                                                                     HOCH.sub.3  CH.sub.2 OTHP                                     HCO.sub.2 CH.sub.2 CHCH.sub.2                                                                   HCH.sub.3   CH.sub.2 OTHP                                     HH               HCH.sub.3   CH.sub.2 OTHP                                     HSCH.sub.2 CH.sub.2 CH.sub.3                                                                    HOCH.sub.3  CH.sub.2 OTHP                                     HSCH.sub.3       HCH.sub.3   CH.sub.2 OTHP                                     HCH(CH.sub.3).sub.2                                                                             HOCH.sub.3  CH.sub.2 OTHP                                     HCH.sub.2 CH.sub.3                                                                              HCH.sub.3   CH.sub.2 OTHP                                     HF               HOCH.sub.3  CH.sub.2 OTHP                                     H Cl             HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OTHP                                     5-ClCl           HCH.sub.2 CH.sub.3                                                                         CH.sub.2 OTHP                                     HBr              HOCH.sub.3  CH.sub.2 OTHP                                     HNO.sub.2        HCH.sub.3   CH.sub.2 OTHP                                     HSO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                          HCH.sub.3   CH.sub.2 OTHP                                     HSO.sub.2 N(CH.sub.3).sub.2                                                                     HOCH.sub.3  CH.sub.2 OTHP                                     HSO.sub.2 N(OCH.sub.3)CH.sub.3                                                                  HOCH.sub.3  CH.sub.2 OTHP                                     HOCH.sub.3       CH.sub.3 CH.sub.3                                                                          CH.sub.2 OTHP                                     5-OCH.sub.3 OCH.sub.3                                                                           HCH.sub.3   CH.sub.2 OTHP                                     5-FO(CH.sub.2).sub.3 CH.sub.3                                                                   HOCH.sub.3  CH.sub.2 OTHP                                     HSO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                            HOCH.sub.3  CH.sub.2 OTHP                                     HSO.sub.2 CH.sub.3                                                                              HCH.sub.3   CH.sub.2 OTHP                                     ______________________________________                                    

                  TABLE 9c                                                         ______________________________________                                          ##STR111##                                                                                                      m.p.                                         R.sub.17                                                                              R.sub.18       R.sub.21 X  Y(°C.)                                ______________________________________                                         H      CO.sub.2 CH.sub.3                                                                             HCH.sub.3   CH.sub.2 OH                                  H      CO.sub.2 CH.sub.2 CH.sub.3                                                                    HOCH.sub.3  CH.sub.2 OH                                  H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  HCH.sub.3   CH.sub.2 OH                                  H      H              HCH.sub.3   CH.sub.2 OH                                  H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                   HOCH.sub.3  CH.sub.2 OH                                  H      SCH.sub.3      CH.sub.3 CH.sub.3                                                                          CH.sub.2 OH                                  H      CH(CH.sub.3).sub.2                                                                            HOCH.sub.3  CH.sub.2 OH                                  H      CH.sub.2 CH.sub.3                                                                             HCH.sub.3   CH.sub.2 OH                                  H      F              HOCH.sub.3  CH.sub.2 OH                                  H      Cl             HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OH                                  5-Cl   Cl             HCH.sub.2 CH.sub.3                                                                         CH.sub.2 OH                                  H      Br             HOCH.sub.3  CH.sub.2 OH                                  H      NO.sub.2       HCH.sub.3   CH.sub.2 OH                                  H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                         HCH.sub.3   CH.sub.2 OH                                  H      SO.sub.2 N(CH.sub.3).sub.2                                                                    HOCH.sub.3  CH.sub.2 OH                                  H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                 HOCH.sub.3  CH.sub.2 OH                                  H      OCH.sub.3      HCH.sub.3   CH.sub.2 OH                                  5-OCH.sub.3                                                                           OCH.sub.3      HCH.sub.3   CH.sub.2 OH                                  5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                    HOCH.sub.3  CH.sub.2 OH                                  H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                           HOCH.sub.3  CH.sub.2 OH                                  H      SO.sub.2 CH.sub.3                                                                             HCH.sub.3   CH.sub.2 OH                                  ______________________________________                                    

                                      TABLE 9d                                     __________________________________________________________________________      ##STR112##                                                                    R.sub.17                                                                            R.sub.18 R.sub.21                                                                          X     Y              m.p.(°C.)                         __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                       H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                              H    CO.sub.2 CH.sub.3                                                                       H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                      H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                            H  CH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                                  H    H        H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                             H    SCH.sub.2 CH.sub.2 CH.sub.3                                                             H  OCH.sub.3                                                                            CH.sub.2 SC.sub.2 H.sub.5                               H    SCH.sub.3                                                                               H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                                H    CH(CH.sub.3).sub.2                                                                      H  OCH.sub.3                                                                            CH.sub.2 OCOC.sub.2 H.sub.5                             H    CH.sub.2 CH.sub.3                                                                       H  CH.sub.3                                                                             CH(OCH(CH.sub. 3)CH.sub.2 O)                            H    F        H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                       H    Cl       H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 SCH.sub.3                                      5-Cl Cl       H  CH.sub.2 CH.sub.3                                                                    CH.sub.2 OCOCH.sub.3                                    H    Br       CH.sub.3                                                                          OCH.sub.3                                                                            CH.sub.2 OCON(CH.sub.3).sub.2                           H    NO.sub.2 H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                                H    SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                     H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                    H    SO.sub.2 N(CH.sub.3).sub.2                                                              H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.2 CH.sub.3                             H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                           H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                              H    OCH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                      5-OCH.sub.3                                                                         OCH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                    5-F  O(CH.sub.2).sub.3 CH.sub.3                                                              H  OCH.sub.3                                                                            CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                    H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                     H  CH.sub.3                                                                             CH.sub.2 OCO( -i-C.sub.3 H.sub.7)                       H    SO.sub.2 CH.sub.3                                                                       H  CH.sub.3                                                                             CH.sub.2 OCONH( -n-C.sub.3 H.sub.7)                     H    Cl       CH.sub.3                                                                          CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                              H    CH.sub.3 H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                              H    Br       H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                              H    SCH.sub.3                                                                               H  OCH.sub.3                                                                            C(CH.sub.3)(OEt).sub.2                                  H    CO.sub.2 CH.sub.3                                                                       H  OCH.sub.3                                                                            C(CH.sub.2 CH.sub.3)(OCH.sub.2 CH.sub.2 CH.sub.2        __________________________________________________________________________                            O)                                                 

                                      TABLE 9e                                     __________________________________________________________________________      ##STR113##                                                                    R.sub.17                                                                            R.sub.18   R.sub.21                                                                          X     Y        m.p.(°C.)                             __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.3                                                                         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                              H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    H          H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SCH.sub.2 CH.sub.2 CH.sub.3                                                               CH.sub.3                                                                          OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    CH(CH.sub.3).sub.2                                                                        H  OCH.sub.2 CH.sub.3                                                                   CH(OCH.sub.3).sub.2                                   H    CH.sub.2 CH.sub.3                                                                         H  CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                   H    F          H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    Cl         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   5-Cl Cl         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    Br         H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    NO.sub.2   H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                     H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(CH.sub.3).sub.2                                                                H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    OCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   5-OCH.sub.3                                                                         OCH.sub.3  H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   5-F  O(CH.sub.2).sub.3 CH.sub.3                                                                H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                       H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.3                                                                         H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                   H    SO.sub.2 CH.sub.2 CH.sub.3                                                                H  CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                          H    NO.sub.2   H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                          H    SO.sub.2 N(CH.sub.3).sub.2                                                                H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                          H    SCH.sub. 2 CH.sub.3                                                                       H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                          H    Br         CH.sub.3                                                                          CH.sub.3                                                                             C(CH.sub.3)(OCH.sub.3).sub.2                          __________________________________________________________________________

                  TABLE 9f                                                         ______________________________________                                          ##STR114##                                                                                                 m.p.                                              R.sub.17 R.sub.18                                                                               R.sub.21 X  Y(°C.)                                     ______________________________________                                         HCO.sub.2 CH.sub.3                                                                              HCH.sub.3   CH.sub.2 OTHP                                     HCO.sub.2 CH.sub.2 CH.sub.3                                                                     HOCH.sub.3  CH.sub.2 OTHP                                     HCO.sub.2 CH.sub.2 CHCH.sub.2                                                                   HCH.sub.3   CH.sub.2 OTHP                                     HH               HCH.sub.3   CH.sub.2 OTHP                                     HSCH.sub.2 CH.sub.2 CH.sub.3                                                                    HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OTHP                                     HSCH.sub.3       HCH.sub.2 CH.sub.3                                                                         CH.sub.2 OTHP                                     HCH(CH.sub.3).sub.2                                                                             HOCH.sub.3  CH.sub.2 OTHP                                     HCH.sub.2 CH.sub.3                                                                              HCH.sub.3   CH.sub.2 OTHP                                     HF               HOCH.sub.3  CH.sub.2 OTHP                                     HCl              HOCH.sub.3  CH.sub.2 OTHP                                     5-ClCl           HCH.sub.3   CH.sub.2 OTHP                                     HBr              HOCH.sub.3  CH.sub.2 OTHP                                     HNO.sub.2        CH.sub.3 CH.sub.3                                                                          CH.sub.2 OTHP                                     HSO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                          HCH.sub.3   CH.sub.2 OTHP                                     HSO.sub.2 N(CH.sub.3).sub.2                                                                     HOCH.sub.3  CH.sub.2 OTHP                                     HSO.sub.2 N(OCH.sub.3)CH.sub.3                                                                  HOCH.sub.3  CH.sub.2 OTHP                                     HOCH.sub.3       HCH.sub.3   CH.sub.2 OTHP                                     5-OCH.sub.3 OCH.sub.3                                                                           HCH.sub.3   CH.sub.2 OTHP                                     5-FO(CH.sub.2).sub.3 CH.sub.3                                                                   HOCH.sub.3  CH.sub.2 OTHP                                     HSO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                            HOCH.sub.3  CH.sub.2 OTHP                                     HSO.sub.2 CH.sub.3                                                                              HCH.sub.3   CH.sub.2 OTHP                                     ______________________________________                                    

                  TABLE 9g                                                         ______________________________________                                          ##STR115##                                                                                                      m.p.                                         R.sub.17                                                                              R.sub.18       R.sub.21 X  Y(°C.)                                ______________________________________                                         H      CO.sub.2 CH.sub.3                                                                             HCH.sub.3   CH.sub.2 OH                                  H      CO.sub.2 CH.sub.2 CH.sub.3                                                                    HOCH.sub.3  CH.sub.2 OH                                  H      CO.sub.2 CH.sub.2 CHCH.sub.2                                                                  HCH.sub.3   CH.sub.2 OH                                  H      H              HCH.sub.3   CH.sub.2 OH                                  H      SCH.sub.2 CH.sub.2 CH.sub.3                                                                   HOCH.sub.3  CH.sub.2 OH                                  H      SCH.sub.3      HCH.sub.3   CH.sub.2 OH                                  H      CH(CH.sub.3).sub.2                                                                            HOCH.sub.3  CH.sub.2 OH                                  H      CH.sub.2 CH.sub.3                                                                             HCH.sub.3   CH.sub.2 OH                                  H      F              HOCH.sub.3  CH.sub.2 OH                                  H      Cl             HOCH.sub.2 CH.sub.3                                                                        CH.sub.2 OH                                  5-Cl   Cl             HCH.sub.2 CH.sub.3                                                                         CH.sub.2 OH                                  H      Br             HOCH.sub.3  CH.sub.2 OH                                  H      NO.sub.2       HCH.sub.3   CH.sub.2 OH                                  H      SO.sub.2 N(CH.sub.3)CH.sub.2 CH.sub.3                                                         CH.sub.3 CH.sub.3                                                                          CH.sub.2 OH                                  H      SO.sub.2 N(CH.sub.3).sub.2                                                                    HOCH.sub.3  CH.sub.2 OH                                  H      SO.sub.2 N(OCH.sub.3)CH.sub.3                                                                 HOCH.sub.3  CH.sub.2 OH                                  H      OCH.sub.3      HCH.sub.3   CH.sub.2 OH                                  5-OCH.sub.3                                                                           OCH.sub.3      HCH.sub.3   CH.sub.2 OH                                  5-F    O(CH.sub.2).sub.3 CH.sub.3                                                                    HOCH.sub.3  CH.sub.2 OH                                  H      SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                           HOCH.sub.3  CH.sub.2 OH                                  H      SO.sub.2 CH.sub.3                                                                             HCH         CH.sub.2 OH                                  ______________________________________                                    

                                      TABLE 9h                                     __________________________________________________________________________      ##STR116##                                                                    R.sub.17                                                                            R.sub.18  R.sub.21                                                                          X     Y           m.p. (°C.)                          __________________________________________________________________________     H    CO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             H    CO.sub.2 CH.sub.3                                                                        CH.sub.3                                                                          OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     H    CO.sub.2 CH.sub.2 CHCH.sub.2                                                             H  CH.sub.3                                                                             CH.sub.2 OCONHCH.sub.3                                 H    H         H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                            H    SCH.sub.2 CH.sub.2 CH.sub.3                                                              H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 SC.sub.2 H.sub.5                              H    SCH.sub.3 H  CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.2 CH.sub.2 O)                               H    CH(CH.sub.3).sub.2                                                                       H  OCH.sub.3                                                                            CH.sub.2 OCOC.sub.2 H.sub.5                            H    CH.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH(OCH(CH.sub.3)CH.sub.2 O)                            H    F         H  OCH.sub.3                                                                            CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                      H    Cl        H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     5-Cl Cl        H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                   H    Br        H  OCH.sub.3                                                                            CH.sub.2 OCON(CH.sub.3).sub.2                          H    NO.sub. 2 H  CH.sub.3                                                                             CH(OCH.sub.2 CH.sub.2 O)                               H    SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                      H  CH.sub.3                                                                             CH.sub.2 OCOCH.sub.3                                   H    SO.sub.2 N(CH.sub.3).sub.2                                                               H  OCH.sub.3                                                                            CH.sub.2 SCH.sub.2 CH.sub.3                            H    SO.sub.2 N(OCH.sub.3)CH.sub.3                                                            H  CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             H    OCH.sub.3 H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 C.sub.2 H.sub.5                     5-OCH.sub.3                                                                         OCH.sub.3 H  CH.sub.3                                                                             CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                   5-F  O(CH.sub.2).sub.3 CH.sub.3                                                               H  OCH.sub.3                                                                            CH.sub.2 OCON(C.sub.2 H.sub.5).sub.2                   H    SO.sub.2 CH.sub.2 CH.sub.2 CH.sub.3                                                      H  CH.sub.3                                                                             CH.sub.2 OCO( .sub.-i-C.sub.3 H.sub.7)                 H    SO.sub.2 CH.sub.3                                                                        H  CH.sub.3                                                                             CH.sub.2 OCONH( -n-C.sub. 3 H.sub.7)                   H    Br        H  CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                             H    NO.sub.2  H  CH.sub.3                                                                             CH(SCH.sub.3).sub.2                                    H    SO.sub.2 N(CH.sub.3)C.sub.2 H.sub.5                                                      H  CH.sub.3                                                                             CH(CH.sub.3)SCH.sub.2 CH.sub.3                         H    OCH.sub.3 H  OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                    H    CO.sub.2 CH.sub.2 CH.sub.3                                                               H  OCH.sub.3                                                                            CH(SCH.sub.2 CH.sub.2 S)                               __________________________________________________________________________

                                      TABLE 10a                                    __________________________________________________________________________      ##STR117##                                                                    R.sub.17                                                                             R.sub.9 R.sub.21                                                                           X     Y         m.p. (°C.)                            __________________________________________________________________________     H     CH.sub.2 CHCH.sub.2                                                                    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     H     CH.sub.3                                                                               H   CH.sub.2 CH.sub.3                                                                    CH.sub.2 OH                                            H     CH.sub.3                                                                               H   OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OCOCH.sub.3                                   H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCONHC.sub.2 H.sub.5                          5-F   C.sub.2 H.sub.5                                                                        H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                    4-Br  CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OTHP                                          4-Br  CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            5-OCH.sub.3                                                                          CH.sub. 3                                                                              H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    5-Cl  CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            5-Cl  CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             5-CH.sub.3                                                                           CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    5-CH.sub.3                                                                           CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OTHP                                          H      .sub.-i-C.sub.3 H.sub.7                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            H     CH.sub.2 CH.sub.2 OCH.sub.3                                                            CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                            H     (CH.sub.2).sub.3 CH.sub.3                                                              H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            H     CH.sub.2 CH.sub.2 Cl                                                                   H   CH.sub.3                                                                             CH.sub.2 OH                                            H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                            H      -n-C.sub.3 H.sub.7                                                                    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                               H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                            H     C.sub.2 H.sub.5                                                                        H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                             H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                             H     CH.sub.3                                                                               H   OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                           H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(SCH.sub.3).sub.2                                    __________________________________________________________________________

                                      TABLE 10b                                    __________________________________________________________________________      ##STR118##                                                                    R.sub.17                                                                             R.sub.9 R.sub.21                                                                           X     Y          m.p. (°C.)                           __________________________________________________________________________     H     CH.sub.2 CHCH.sub.2                                                                    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               CH.sub.3                                                                           CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     H     CH.sub.3                                                                               H   CH.sub.2 CH.sub.3                                                                    CH.sub.2 OH                                            H     CH.sub.3                                                                               H   OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OCOCH.sub.3                                   H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCONHC.sub.2 H.sub.5                          5-F   C.sub.2 H.sub.5                                                                        H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                    4-Br  CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OTHP                                          4-Br  CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            5-OCH.sub.3                                                                          CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    5-Cl  CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            5-Cl  CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             5-CH.sub.3                                                                           CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    5-CH.sub.3                                                                           CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OTHP                                          H      .sub.-i-C.sub.3 H.sub.7                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            H     CH.sub.2 CH.sub.2 OCH.sub.3                                                            H   CH.sub.3                                                                             CH.sub.2 OH                                            H     (CH.sub.2).sub.3 CH.sub.3                                                              H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            H     CH.sub.2 CH.sub.2 Cl                                                                   H   CH.sub.3                                                                             CH.sub.2 OH                                            H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                            H      -n-C.sub.3 H.sub.7                                                                    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                               H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                            H     C.sub.2 H.sub.5                                                                        H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                             H     CH.sub.2 CH.sub.3                                                                      H   CH.sub.3                                                                             CH(SCH.sub.2 CH.sub.3).sub.2                           H     CH.sub.3                                                                               H   OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.2 CH.sub.2 O)                      H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                             __________________________________________________________________________

                                      TABLE 10c                                    __________________________________________________________________________      ##STR119##                                                                    R.sub.17                                                                            R.sub.9 R.sub.21                                                                           X     Y            m.p. (°C.)                          __________________________________________________________________________     H    CH.sub.2 CHCH.sub.2                                                                    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     H    CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                              H    CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                      H    CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OH                                             H    CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                    H    CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCONHC.sub.2 H.sub.5                           2-F  C.sub.2 H.sub.5                                                                        H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     5-Br CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OTHP                                           5-Br CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                             2-OCH.sub.3                                                                         CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     2-Cl CH.sub.3                                                                               H   OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OH                                             2-Cl CH.sub.3                                                                               H   CH.sub.2 CH.sub.3                                                                    CH(OC.sub.2 H.sub.5).sub.2                              5-CH.sub.3                                                                          CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     5-CH.sub.3                                                                          CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OTHP                                           H     .sub.-i-C.sub.3 H.sub.7                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                             H    CH.sub.2 CH.sub.2 OCH.sub.3                                                            CH.sub.3                                                                           CH.sub.3                                                                             CH.sub.2 OH                                             H    (CH.sub.2).sub.3 CH.sub.3                                                              H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     H    CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                     H    CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                             H    CH.sub.2 CH.sub.2 Cl                                                                   H   CH.sub.3                                                                             CH.sub.2 OH                                             H    CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                             H     -n-C.sub.3 H.sub.7                                                                    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     H    CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                H    CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                             H    C.sub.2 H.sub.5                                                                        H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                     H    CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(OC.sub.2 H.sub. 5).sub.2                             H    CH.sub.2 CH.sub.3                                                                      H   OCH.sub.3                                                                            CH.sub.2 SO.sub.2 CH.sub.3                              H    CH.sub.3                                                                               CH.sub.3                                                                           OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                            H    CH.sub.3                                                                               H   OCH.sub.3                                                                            C(CH.sub.2 CH.sub.3)(OCH.sub.2 CH.sub.2 O)              __________________________________________________________________________

                                      TABLE 10d                                    __________________________________________________________________________      ##STR120##                                                                    R.sub.17                                                                             R.sub.9 R.sub.21                                                                           X     Y         m.p. (°C.)                            __________________________________________________________________________     H     CH.sub.2 CHCH.sub.2                                                                    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OH                                            H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                   H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCONHC.sub.2 H.sub.5                          5-F   C.sub.2 H.sub.5                                                                        H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                    4-Br  CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OTHP                                          4-Br  CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            5-OCH.sub. 3                                                                         CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    5-Cl  CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            5-Cl  CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             5-CH.sub.3                                                                           CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    5-CH.sub.3                                                                           CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OTHP                                          H      .sub.-i-C.sub.3 H.sub.7                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            H     CH.sub.2 CH.sub.2 OCH.sub.3                                                            H   CH.sub.2 CH.sub.3                                                                    CH.sub.2 OH                                            H     (CH.sub.2).sub.3 CH.sub.3                                                              H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               CH.sub.3                                                                           OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            H     CH.sub.2 CH.sub.2 Cl                                                                   H   CH.sub.3                                                                             CH.sub.2 OH                                            H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                            H      -n-C.sub.3 H.sub.7                                                                    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                               H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                            H     C.sub.2 H.sub.5                                                                        H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.2 CH.sub.3                                                                   CH(OC.sub.2 H.sub.5).sub.2                             H     CH.sub.2 CH.sub.3                                                                      H   OCH.sub.3                                                                            CH(SCH.sub.2 CH.sub.3).sub.2                           H     CH.sub.3                                                                               H   OC.sub.2 H.sub.5                                                                     CH.sub.2 SO.sub.2 CH.sub.2 CH.sub.3                    H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH(CH.sub.3)(SCH.sub.3)                                __________________________________________________________________________

                                      TABLE 10e                                    __________________________________________________________________________      ##STR121##                                                                    R.sub.17                                                                             R.sub.9 R.sub.21                                                                           X     Y         m.p. (°C.)                            __________________________________________________________________________     H     CH.sub.2 CHCH.sub.2                                                                    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               CH.sub.3                                                                           CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             H     CH.sub.3                                                                               CH.sub.3                                                                           OCH.sub.3                                                                            CH.sub.2 SCH.sub.3                                     H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OH                                            H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                   H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCONHC.sub.2 H.sub.5                          5-F   C.sub.2 H.sub.5                                                                        H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                    4-Br  CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OTHP                                          4-Br  CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub. 2 OH                                           5-OCH.sub.3                                                                          CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    5-Cl  CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            5-Cl  CH.sub.3                                                                               H   CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                             5-CH.sub.3                                                                           CH.sub.3                                                                               H   CH.sub.2 CH.sub.3                                                                    CH(OCH.sub.3).sub.2                                    5-CH.sub.3                                                                           CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OTHP                                          H      .sub.-i-C.sub.3 H.sub.7                                                               H   OCH.sub.2 CH.sub.3                                                                   CH.sub.2 OH                                            H     CH.sub.2 CH.sub.2 OCH.sub.3                                                            H   CH.sub.3                                                                             CH.sub.2 OH                                            H     (CH.sub.2).sub.3 CH.sub.3                                                              H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH.sub.2 OH                                            H     CH.sub.2 CH.sub.2 Cl                                                                   H   CH.sub.3                                                                             CH.sub.2 OH                                            H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                            H      -n-C.sub.3 H.sub.7                                                                    H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                               H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                            H     C.sub.2 H.sub.5                                                                        H   CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                    H     CH.sub.3                                                                               H   OCH.sub. 3                                                                           CH(OC.sub.2 H.sub.5).sub.2                             H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 SCH.sub.2 CH.sub.3                            H     CH.sub.3                                                                               H   OCH.sub.3                                                                            CH(CH.sub.3)SCH.sub.3                                  H     CH.sub.3                                                                               H   CH.sub.3                                                                             CH.sub.2 SO.sub.2 CH.sub.3                             __________________________________________________________________________

                                      TABLE 10f                                    __________________________________________________________________________      ##STR122##                                                                    R.sub.17                                                                            R.sub.9 R.sub.21                                                                          X     Y           m.p. (°C.)                            __________________________________________________________________________     H    CH.sub.2 CHCH.sub.2                                                                    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  CH.sub.2 CH.sub.3                                                                    CH(OC.sub.2 H.sub.5).sub.2                               H    CH.sub.3                                                                               H  OCH.sub.2 CH.sub.3                                                                   CH.sub.2 SCH.sub.3                                       H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OH                                              H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OCOCH.sub.3                                     H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCONHC.sub.2 H.sub.5                            2-F  C.sub.2 H.sub.5                                                                        H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      5-Br CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OTHP                                            5-Br CH.sub. 3                                                                              H  OCH.sub.3                                                                            CH.sub.2 OH                                              2-OCH.sub.3                                                                         CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      2-Cl CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              2-Cl CH.sub.3                                                                               CH.sub.3                                                                          CH.sub.3                                                                             CH(OC.sub.2 H.sub.5).sub.2                               5-CH.sub.3                                                                          CH.sub.3                                                                               H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      5-CH.sub.3                                                                          CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OTHP                                            H     .sub.-i-C.sub.3 H.sub.7                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              H    CH.sub.2 CH.sub.2 OCH.sub.3                                                            H  CH.sub.3                                                                             CH.sub.2 OH                                              H    (CH.sub.2).sub.3 CH.sub.3                                                              H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH.sub.2 OH                                              H    CH.sub.2 CH.sub.2 Cl                                                                   H  CH.sub.3                                                                             CH.sub.2 OH                                              H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCOC.sub.2 H.sub.5                              H     -n-C.sub.3 H.sub.7                                                                    H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(OCH.sub.2 CH.sub.2 O)                                 H    CH.sub.3                                                                               H  CH.sub.3                                                                             CH.sub.2 OCO.sub.2 CH.sub.3                              H    C.sub.2 H.sub.5                                                                        H  CH.sub.3                                                                             CH(OCH.sub.3).sub.2                                      H    CH.sub. 3                                                                              H  OCH.sub.3                                                                            CH(OC.sub.2 H.sub.5).sub.2                               H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(SCH.sub.2 CH.sub.2 S)                                 H    CH.sub.3                                                                               H  OCH.sub.3                                                                            CH(OCH(CH.sub.3)CH.sub.2 O)                              H    CH.sub.3                                                                               H  OCH.sub.3                                                                            C(CH.sub.3)(OCH.sub.3).sub.2                             __________________________________________________________________________

                  TABLE 11a                                                        ______________________________________                                          ##STR123##                                                                    R.sub.18                                                                             R.sub.21                                                                              X          Y            m.p. (°C.)                         ______________________________________                                         H     H      CH.sub.3   CH(OCH.sub.3).sub.2                                    H     H      CH.sub.3   CH.sub.2 OTHP                                          H     H      OCH.sub.2 CH.sub.3                                                                        CH.sub.2 OH                                            H     H      OCH.sub.3  CH(OCH.sub.2 CH.sub.2 O)                               Cl    H      CH.sub.3   CH(OCH.sub.3).sub.2                                    Cl    H      CH.sub.2 CH.sub.3                                                                         CH(OC.sub.2 H.sub.5).sub.2                             Cl    H      CH.sub.3   CH.sub.2 OH                                            Cl    H      CH.sub.3   CH.sub.2 OTHP                                          Cl    CH.sub.3                                                                              OCH.sub.3  CH(OCH.sub.3).sub.2                                    Cl    H      OCH.sub.3  CH.sub.2 OCOCH.sub.3                                   Cl    H      OCH.sub.3  CH.sub.2 OH                                            Br    H      CH.sub.3   CH(OCH.sub.3).sub.2                                    Br    H      CH.sub.3   CH(OC.sub.2 H.sub.5).sub.2                             Br    H      CH.sub.3   CH.sub. 2 OH                                           Br    H      OCH.sub.3  CH.sub.2 OH                                            Br    H      OCH.sub.3  CH.sub.2 OCO.sub.2 CH.sub.3                            CH.sub.3                                                                             H      CH.sub.3   CH(OCH.sub.3).sub.2                                    CH.sub.3                                                                             H      CH.sub.3   CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                      CH.sub.3                                                                             H      CH.sub.3   CH.sub.2 OH                                            CH.sub.3                                                                             H      CH.sub.3   CH.sub.2 OCONHC.sub.2 H.sub.5                          CH.sub.3                                                                             H      OCH.sub.3  CH(OCH.sub.3).sub.2                                    CH.sub.3                                                                             H      OCH.sub.3  CH.sub.2 OTHP                                          CH.sub.3                                                                             H      OCH.sub.3  CH.sub.2 OCOCH.sub.3                                   CH.sub.3                                                                             H      OCH.sub.3  CH.sub.2 OH                                            Cl    H      CH.sub.3   CH.sub.2 SO.sub.2 CH.sub.3                             Br    H      OCH.sub.3  CH(SCH.sub.3).sub.2                                    CH.sub.3                                                                             H      OCH.sub.3  C(CH.sub.3)(OCH.sub.3).sub.2                           ______________________________________                                    

                  TABLE 11b                                                        ______________________________________                                          ##STR124##                                                                    R.sub.18                                                                             R.sub.21                                                                              X          Y            m.p. (°C.)                         ______________________________________                                         H     H      CH.sub.3   CH(OCH.sub.3).sub.2                                    H     H      CH.sub.3   CH.sub.2 OTHP                                          H     H      OCH.sub.3  CH.sub.2 OH                                            H     H      OCH.sub.3  CH(OCH.sub.2 CH.sub.2 O)                               Cl    H      CH.sub.2 CH.sub.3                                                                         CH(OCH.sub.3).sub.2                                    Cl    H      CH.sub.3   CH(OC.sub.2 H.sub.5).sub.2                             Cl    CH.sub.3                                                                              CH.sub.3   CH.sub.2 OH                                            Cl    H      CH.sub.3   CH.sub.2 OTHP                                          Cl    H      OCH.sub.3  CH(OCH.sub.3).sub.2                                    Cl    H      OCH.sub.3  CH.sub.2 OCOCH.sub.3                                   Cl    H      OCH.sub.3  CH.sub.2 OH                                            Br    H      CH.sub.3   CH(OCH.sub.3).sub.2                                    Br    H      CH.sub.3   CH(OC.sub.2 H.sub.5).sub.2                             Br    H      CH.sub.3   CH.sub.2 OH                                            Br    H      OCH.sub.3  CH.sub.2 OH                                            Br    H      OCH.sub.2 CH.sub.3                                                                        CH.sub.2 OCO.sub.2 CH.sub.3                            CH.sub.3                                                                             H      CH.sub.3   CH(OCH.sub.3).sub.2                                    CH.sub.3                                                                             H      CH.sub.3   CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                      CH.sub.3                                                                             H      CH.sub.3   CH.sub.2 OH                                            CH.sub.3                                                                             H      CH.sub.3   CH.sub.2 OCONHC.sub.2 H.sub.5                          CH.sub.3                                                                             H      OCH.sub.3  CH(OCH.sub.3).sub.2                                    CH.sub.3                                                                             H      OCH.sub.3  CH.sub.2 OTHP                                          CH.sub.3                                                                             H      OCH.sub.3  CH.sub.2 OCOCH.sub.3                                   CH.sub.3                                                                             H      OCH.sub.3  CH.sub.2 OH                                            Cl    H      CH.sub.3   CH.sub.2 SO.sub.2 CH.sub.3                             Br    H      CH.sub.3   CH(SCH.sub.3).sub.2                                    CH.sub.3                                                                             H      CH.sub.3   CH(SCH.sub.2 CH.sub.3).sub.2                           ______________________________________                                    

                                      TABLE 12                                     __________________________________________________________________________      ##STR125##                                                                    R.sub.19   R.sub.21                                                                           X   Y           Z   m.p. (°C.)                           __________________________________________________________________________     Cl         H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              Cl         CH.sub.3                                                                           CH.sub.3                                                                           CH.sub.2 OCOCH.sub.3                                                                       CH                                              Cl         H   CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                                                   Z                                               Cl         H   OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         Z                                               Cl         H   OCH.sub.3                                                                          CH(OEt).sub.2                                                                              CH                                              NO.sub.2   H   C.sub.2 H.sub.5                                                                    CH(SCH.sub.2 CH.sub.2 S)                                                                   CH                                              NO.sub.2   H   CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          CH                                              NO.sub.2   H   Cl  CH(OCH.sub.3).sub.2                                                                        CH                                              NO.sub.2   H   CH.sub.3                                                                           CH(OCH(CH.sub.3)CH.sub.2 O)                                                                Z                                               NO.sub.2   H   OCH.sub.3                                                                          CH.sub.2 SEt                                                                               CH                                              NO.sub.2   H   OCH.sub.3                                                                          CH.sub.2 OH CH                                              CF.sub.3   H   OC.sub.2 H.sub.5                                                                   CH.sub.2 OTHP                                                                              CH3                                             CF.sub.3   H   CH.sub.3                                                                           CH.sub.2 OCON(CH.sub.3).sub.2                                                              CH                                              CF.sub.3   H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              CF.sub.3   H   CH.sub.3                                                                           CH(OEt).sub.2                                                                              Z                                               CF.sub.3   H   OCH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                                                          CH                                              OCH.sub.3  CH.sub.3                                                                           OCH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                                                                CH                                              OCH.sub.3  H   OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                              OCH.sub.3  H   OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        CH                                              OCH.sub.3  H   CH.sub.3                                                                           CH(OEt).sub.2                                                                              Z                                               OCH.sub.3  H   CH.sub.3                                                                           CH.sub.2 SCH.sub.3                                                                         CH                                              OCH.sub.3  H   CH.sub.3                                                                           CH.sub.2 SEt                                                                               CH                                              OCH.sub.3  H   CH.sub.3                                                                           CH.sub.2 OCONHCH.sub.3                                                                     CH                                              CO.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                           CH.sub.2 SEt                                                                               CH                                              CO.sub.2 CH.sub.3                                                                         CH.sub.3                                                                           CH.sub.3                                                                           CH(OEt).sub.2                                                                              Z                                               CO.sub.2 CH.sub.3                                                                         CH.sub.3                                                                           CH.sub.3                                                                           CH(SCH.sub.2 CH.sub.2 S)                                                                   CH                                              Cl         H   OCH.sub.3                                                                          CH(SCH.sub.3).sub.2                                                                        CH                                              NO.sub.2   H   CH.sub.3                                                                           CH.sub.2 SO.sub.2 CH.sub.3                                                                 CH                                              CO.sub.2 CH.sub.3                                                                         H   OCH.sub.3                                                                          C(CH.sub.3)(OCH.sub.3).sub.2                                                               CH                                              CO.sub.2 CH.sub.3                                                                         CH.sub.3                                                                           OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                              CO.sub.2 CH.sub. 3                                                                        CH.sub.3                                                                           OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        CH                                              CO.sub.2 CH.sub.3                                                                         CH.sub.3                                                                           OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          Z                                               CO.sub.2 CH.sub.2 CH.sub.3                                                                CH.sub.3                                                                           C.sub.2 H.sub.5                                                                    CH(OCH.sub.3).sub.2                                                                        CH                                              CO.sub.2 CH.sub.2 CH.sub.3                                                                CH.sub.3                                                                           OC.sub.2 H.sub.5                                                                   CH(OCH.sub.3).sub.2                                                                        CH                                              CO.sub.2 CH.sub.2 CH.sub.3                                                                CH.sub.3                                                                           OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        CH                                              CO.sub.2 -n-C.sub.4 H.sub.9                                                               CH.sub.3                                                                           OCH.sub.3                                                                          CH.sub.2 OH CH                                              CO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          CH.sub.3                                                                           OCH.sub.3                                                                          CH.sub.2 OH Z                                               SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             CH.sub.3                                                                           OCH.sub.3                                                                          CH.sub.2 OH CH                                              SO.sub.2 N(CH.sub.3).sub.2                                                                H   CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                              SO.sub.2 N(CH.sub.3).sub.2                                                                CH.sub.3                                                                           CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                              SO.sub.2 N(CH.sub.3).sub.2                                                                H   CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                                                   Z                                               SO.sub.2 N(CH.sub.3).sub.2                                                                H   CH.sub.3                                                                           CH.sub.2 OCOCH.sub.3                                                                       CH                                              SO.sub.2 N(CH.sub.3).sub.2                                                                H   OCH.sub.3                                                                          CH.sub.2 OCO.sub.2 CH.sub. 3                                                               CH                                              SO.sub.2 N(CH.sub.3).sub.2                                                                H   OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         CH                                              SO.sub.2 N(CH.sub.3).sub.2                                                                H   OCH.sub.3                                                                          CH.sub.2 OTHP                                                                              CH                                              SO.sub.2 (CH.sub.2 CH.sub.3)CH.sub.3                                                      H   OCH.sub.3                                                                          CH.sub.2 OH Z                                               SO.sub.2 (CH.sub.2 CH.sub.3)CH.sub.3                                                      H   CH.sub.3                                                                           CH.sub.2 OH CH                                              OSO.sub.2 CH.sub.3                                                                        H   CH.sub.3                                                                           CH.sub.2 OH CH                                              OSO.sub.2 CH.sub.3                                                                        H   CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.3).sub.2                                                               CH                                              OSO.sub.2 CH.sub.3                                                                        H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              OSO.sub.2 CH.sub.3                                                                        H   OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        CH                                              OSO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                     H   OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        Z                                               OSO.sub.2 CH.sub.2 CF.sub.3                                                               H   OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                              SCH.sub.3  H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              SCH.sub.3  CH.sub.3                                                                           CH.sub.3                                                                           CH.sub.2 OCOC.sub.2 H.sub.5                                                                Z                                               SCH.sub.3  H   OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   Z                                               SCH.sub.2 CH.sub.3                                                                        H   OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         CH                                              SCH.sub.2 CH.sub.3                                                                        H   Cl  CH(OEt).sub.2                                                                              CH                                              SO.sub.2 CH.sub.3                                                                         CH.sub.3                                                                           OCH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 S)                                                                   Z                                               SO.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          CH                                              SO.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              SO.sub.2  -n-C.sub.3 H.sub.7                                                              H   C.sub.2 H.sub.5                                                                    CH(OCH(CH.sub.3)CH.sub.2 O)                                                                CH                                              SO.sub.2  -n-C.sub.3 H.sub.7                                                              H   OCH.sub.3                                                                          CH.sub.2 SEt                                                                               Z                                               SO.sub.2  -n-C.sub.3 H.sub.7                                                              H   OCH.sub.3                                                                          CH.sub.2 OH CH                                              SO.sub.2 CH.sub.2 CHCH.sub.2                                                              H   OCH.sub.3                                                                          CH.sub.2 OTHP                                                                              CH                                              SO.sub.2 -n-C.sub.4 H.sub.9                                                               H   OCH.sub.3                                                                          CH.sub.2 OH CH                                              S .sub.-t-C.sub.4 H.sub.9                                                                 H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              OCH.sub.2 CH.sub.2 Cl                                                                     H   CH.sub.3                                                                           CH.sub.2 OCON(CH.sub.3).sub.2                                                              CH                                              OCHFCHF.sub.2                                                                             H   OC.sub.2 H.sub.5                                                                   CH.sub.2 OCO.sub.2 Et                                                                      Z                                               OCH.sub.2 CF.sub.3                                                                        H   OCH.sub.3                                                                          CH.sub.2 OCO.sub.2 CH.sub.3                                                                CH                                              O -n-C.sub.3 H.sub.7                                                                      H   OCH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                                                          CH                                              O -n-C.sub.3 H.sub.7                                                                      H   OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          CH                                              O -n-C.sub.3 H.sub.7                                                                      H   Cl  CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          CH                                              O -n-C.sub.4 H.sub.9                                                                      H   OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          Z                                               O -n-C.sub.4 H.sub.9                                                                      H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              OCH.sub.2 CH.sub.3                                                                        H   CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.3).sub.2                                                               CH                                              OCH.sub.2 CH.sub.3                                                                        H   CH.sub.3                                                                           CH.sub.2 OH CH                                              OCF.sub.3  CH.sub.3                                                                           OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   CH.sub.3                                        OCF.sub.3  H   OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         Z                                               OCF.sub.3  H   OCH.sub.3                                                                          CH.sub.2 OH CH                                              CH.sub.2 Cl                                                                               H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              CH.sub.2 Cl                                                                               H   OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        N                                               __________________________________________________________________________

                                      TABLE 13                                     __________________________________________________________________________      ##STR126##                                                                    R.sub.20   R.sub.21                                                                           X   Y           Z   m.p. (°C.)                           __________________________________________________________________________     Cl         H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              Cl         CH.sub.3                                                                           CH.sub.3                                                                           CH.sub.2 OCOCH.sub.3                                                                       CH                                              Cl         H   CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                                                   Z                                               Cl         H   OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         Z                                               Cl         H   OCH.sub.3                                                                          CH(OEt).sub.2                                                                              CH                                              NO.sub.2   H   C.sub.2 H.sub.5                                                                    CH(SCH.sub.2 CH.sub.2 S)                                                                   CH                                              NO.sub.2   H   CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          CH                                              NO.sub.2   H   Cl  CH(OCH.sub.3).sub.2                                                                        CH                                              NO.sub.2   H   CH.sub.3                                                                           CH(OCH(CH.sub.3)CH.sub.2 O)                                                                Z                                               NO.sub.2   H   OCH.sub.3                                                                          CH.sub.2 SEt                                                                               CH                                              NO.sub.2   H   OCH.sub.3                                                                          CH.sub.2 OH CH                                              CF.sub.3   H   OC.sub.2 H.sub.5                                                                   CH.sub.2 OTHP                                                                              CH                                              CF.sub.3   H   CH.sub.3                                                                           CH.sub.2 OCON(CH.sub.3).sub.2                                                              CH                                              CF.sub.3   H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              CF.sub.3   H   CH.sub.3                                                                           CH(OEt).sub.2                                                                              Z                                               CF.sub.3   H   OCH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                                                          CH                                              OCH.sub.3  CH.sub.3                                                                           OCH.sub.3                                                                          CH(OCH(CH.sub.3)CH.sub.2 O)                                                                CH                                              OCH.sub.3  H   OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                              OCH.sub.3  H   OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        CH                                              OCH.sub.3  H   CH.sub.3                                                                           CH(OEt).sub.2                                                                              Z                                               OCH.sub.3  H   CH.sub.3                                                                           CH.sub.2 SCH.sub.3                                                                         CH                                              OCH.sub.3  H   CH.sub.3                                                                           CH.sub.2 SEt                                                                               CH                                              OCH.sub.3  H   CH.sub.3                                                                           CH.sub.2 OCONHCH.sub.3                                                                     CH                                              CO.sub.2 CH.sub.3                                                                         H   CH.sub.3                                                                           CH.sub.2 SEt                                                                               CH                                              CO.sub.2 CH.sub.3                                                                         CH.sub.3                                                                           CH.sub.3                                                                           CH(OEt).sub.2                                                                              Z                                               CO.sub.2 CH.sub.3                                                                         CH.sub.3                                                                           CH.sub.3                                                                           CH(SCH.sub.2 CH.sub.2 S)                                                                   CH                                              CO.sub.2 CH.sub.3                                                                         CH.sub.3                                                                           OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                              CO.sub.2 CH.sub.3                                                                         CH.sub.3                                                                           OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        CH                                              CO.sub.2 CH.sub.3                                                                         CH.sub.3                                                                           OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          Z                                               CO.sub.2 CH.sub.2 CH.sub.3                                                                CH.sub.3                                                                           C.sub.2 H.sub. 5                                                                   CH(OCH.sub.3).sub.2                                                                        CH                                              CO.sub.2 CH.sub.2 CH.sub.3                                                                CH.sub.3                                                                           OC.sub.2 H.sub.5                                                                   CH(OCH.sub.3).sub.2                                                                        CH                                              CO.sub.2 CH.sub.2 CH.sub.3                                                                CH.sub.3                                                                           OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        CH                                              CO.sub.2 -n-C.sub.4 H.sub.9                                                               CH.sub.3                                                                           OCH.sub.3                                                                          CH.sub.2 OH CH                                              CO.sub.2 .sub.-i-C.sub.3 H.sub.7                                                          CH.sub.3                                                                           OCH.sub.3                                                                          CH.sub.2 OH Z                                               SO.sub.2 N(OCH.sub.3)CH.sub.3                                                             CH.sub.3                                                                           OCH.sub.3                                                                          CH.sub.2 OH CH                                              SO.sub.2 N(CH.sub.3).sub.2                                                                H   CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                              SO.sub.2 N(CH.sub.3).sub.2                                                                CH.sub.3                                                                           CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                              SO.sub.2 N(CH.sub.3).sub.2                                                                H   CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.2 O)                                                                   Z                                               SO.sub.2 N(CH.sub.3).sub.2                                                                H   CH.sub.3                                                                           CH.sub.2 OCOCH.sub.3                                                                       CH                                              SO.sub.2 N(CH.sub.3).sub.2                                                                H   OCH.sub.3                                                                          CH.sub.2 OCO.sub.2 CH.sub.2                                                                CH                                              SO.sub.2 N(CH.sub.3).sub.2                                                                H   OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         CH                                              SO.sub.2 N(CH.sub.3).sub.2                                                                H   OCH.sub.3                                                                          CH.sub.2 OTHP                                                                              CH                                              OSO.sub.2 CH.sub.3                                                                        H   CH.sub.3                                                                           CH.sub.2 OH CH                                              OSO.sub.2 CH.sub.3                                                                        H   CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.3).sub.2                                                               CH                                              OSO.sub.2 CH.sub.3                                                                        H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              OSO.sub.2 CH.sub.3                                                                        H   OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        CH                                              OSO.sub.2 CH.sub.2 CH.sub.2 OCH.sub.3                                                     H   OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        Z                                               OSO.sub.2 CH.sub.2 CF.sub.3                                                               H   OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                              CH.sub.3   H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              CH.sub.3   CH.sub.3                                                                           CH.sub.3                                                                           CH.sub.2 OCOC.sub.2 H.sub.5                                                                Z                                               CH.sub.3   H   OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   Z                                               CH.sub.2 CH.sub.3                                                                         H   OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         CH                                              CH.sub.2 CH.sub.3                                                                         H   Cl  CH(OEt).sub.2                                                                              CH                                              CH.sub.3   H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                               -n-C.sub.3 H.sub.7                                                                       H   C.sub.2 H.sub.5                                                                    CH(OCH(CH.sub.3)CH.sub.2 O)                                                                CH                                               -n-C.sub.3 H.sub.7                                                                       H   OCH.sub.3                                                                          CH.sub.2 SEt                                                                               Z                                                -n-C.sub.3 H.sub.7                                                                       H   OCH.sub.3                                                                          CH.sub.2 OH CH                                               -n-C.sub.4 H.sub.9                                                                       H   OCH.sub.3                                                                          CH.sub.2 OH CH                                              C.sub.4 H.sub.9                                                                           H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              OCH.sub.2 CH.sub.2 Cl                                                                     H   CH.sub.3                                                                           CH.sub.2 OCON(CH.sub.3).sub.2                                                              CH                                              OCHFCHF.sub.2                                                                             H   OC.sub.2 H.sub.5                                                                   CH.sub.2 OCO.sub.2 Et                                                                      Z                                               OCH.sub.2 CF.sub.3                                                                        H   OCH.sub.3                                                                          CH.sub.2 OCO.sub.2 CH.sub.3                                                                CH                                              O -n-C.sub.3 H.sub.7                                                                      H   OCH.sub.3                                                                          CH(SCH.sub.2 CH.sub.2 CH.sub.2 S)                                                          CH                                              O -n-C.sub.3 H.sub.7                                                                      H   OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          CH                                              O -n-C.sub.3 H.sub.7                                                                      H   Cl  CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          CH                                              O -n-C.sub.4 H.sub.9                                                                      H   OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 CH.sub.2 O)                                                          Z                                               O -n-C.sub.4 H.sub.9                                                                      H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              OCH.sub.2 CH.sub.3                                                                        H   CH.sub.3                                                                           CH(OCH.sub.2 CH.sub.3).sub.2                                                               CH                                              OCH.sub.2 CH.sub.3                                                                        H   CH.sub.3                                                                           CH.sub.2 OH CH                                              OCF.sub.3  CH.sub.3                                                                           OCH.sub.3                                                                          CH(OCH.sub.2 CH.sub.2 O)                                                                   CH                                              OCF.sub.3  H   OCH.sub.3                                                                          CH.sub.2 SCH.sub.3                                                                         Z                                               OCF.sub.3  H   OCH.sub.3                                                                          CH.sub.2 OH CH                                              CH.sub.2 Cl                                                                               H   CH.sub.3                                                                           CH(OCH.sub.3).sub.2                                                                        CH                                              CH.sub.2 Cl                                                                               H   OCH.sub.3                                                                          CH(OCH.sub.3).sub.2                                                                        CH                                              __________________________________________________________________________

FORMULATIONS

Useful formulations of the compounds of Formula I can be prepared in conventional ways. They include dusts, granules, pellets, solutions, suspensions, emulsions, wettable powders, emulsifiable concentrates and the like. Many of these may be applied directly. Sprayable formulations can be extended in suitable media and used at spray volumes of from a few liters to several hundred liters per hectare. High strength compositions are primarily used as intermediates for further formulation. The formulations, broadly, can contain from about 0.1% to 99% by weight of active ingredient(s) and at least one of (a) about 0.1% to 20% surfactant(s) and (b) about 1% to 99.9% solid or liquid inert diluent(s). More specifically, they will contain these ingredients in the following approximate proportions:

                  TABLE 14                                                         ______________________________________                                                     Active  Weight Percent*                                                        Ingredient                                                                             Diluent(s)                                                                               Surfactant(s)                                    ______________________________________                                         Wettable Powders                                                                             20-90      0-74     1-10                                         Oil Suspensions,                                                                              3-50     40-95     0-15                                         Emulsions, Solutions,                                                          (including Emulsifiable                                                        Concentrates)                                                                  Aqueous Suspension                                                                           10-50     40-84     1-20                                         Dusts          1-25     70-99     0-5                                          Granules and Pellets                                                                         0.1-95      5-99.9  0-15                                         High Strength 90-99      0-10     0-2                                          Compositions                                                                   ______________________________________                                          *Active ingredient plus at least one of a Surfactant or a Diluent equals       100 weight percent.                                                      

Lower or higher levels of active ingredient can, of course, be present depending on the intended use and the physical properties of the compound. Higher ratios of surfactant to active ingredient are sometimes desirable, and are achieved by incorporation into the formulation or by tank mixing.

Typical solid diluents are described in Watkins, et al., "Handbook of Insecticide Dust Diluents and Carriers", 2nd Ed., Dorland Books, Caldwell, N.J., but other solids, either mined or manufactured, may be used. The more absorptive diluents are preferred for wettable powders and the denser ones for dusts. Typical liquid diluents and solvents are described in Marsden, "Solvents Guide," 2nd Ed., Interscience, N.Y., 1950. Solubility under 0.1% is preferred for suspension concentrates; solution concentrates are preferably stable against phase separation at 0° C. "McCutcheon's Detergents and Emulsifiers Annual", MC Publishing Corp., Ridgewood, N.J., as well as Sisely and Wood, "Encyclopedia of Surface Active Agents", Chemical Publishing Co., Inc., New York, 1964, list surfactants and recommended uses. All formulations can contain minor amounts of additives to reduce foaming, caking, corrosion, microbiological growth, etc.

The methods of making such compositions are well known. Solutions are prepared by simply mixing the ingredients. Fine solid compositions are made by blending and, usually, grinding as in a hammer or fluid energy mill. Suspensions are prepared by wet milling (see, for example, Littler, U.S. Pat. No. 3,060,084). Granules and pellets may be made by spraying the active material upon preformed granular carriers or by agglomeration techniques. See J. E. Browning, "Agglomeration", Chemical Engineering, Dec. 4, 1967, pp. 147ff. and "Perry's Chemical Engineer's Handbook", 5th Ed., McGraw-Hill, New York 1973, pp. 8-57ff.

For further information regarding the art of formulation, see for example:

H. M. Loux, U.S. Pat. No. 3,235,361, Feb. 15, 1966, Col. 6, line 16 through Col. 7, line 19 and Example 10 through 41;

R. W. Luckenbaugh, U.S. Pat. No. 3,309,192, Mar. 14, 1967, Col. 5, line 43 through Col. 7, line 62 and Examples 8, 12, 15, 39, 41, 52, 53, 58, 132, 138-140, 162-164, 166, 167 and 169-182;

H. Gysin and E. Knusli, U.S. Pat. No. 2,891,855, June 23, 1959, Col. 3, line 66 through Col 5, line 17 and Examples 1-4;

G. C. Klingman, "Weed Control as a Science", John Wiley & Sons, Inc., New York, 1961, pp. 81-96; and

J. D. Fryer and S. A. Evans, "Weed Control Handbook", 5th Ed., Blackwell Scientific Publications, Oxford, 1968, pp. 101-103.

In the following examples, all parts are by weight unless otherwise indicated.

EXAMPLE 7 Wettable Powder

    ______________________________________                                         3-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)-                                                           80%                                                 aminocarbonyl]aminosulfonyl]-2-thiophene-                                      carboxylic acid, methyl ester                                                  sodium alkylnaphthalenesulfonate                                                                           2%                                                 sodium ligninsulfonate      2%                                                 synthetic amorphous silica  3%                                                 kaolinite                  13%                                                 ______________________________________                                    

The ingredients are blended, hammer-milled until all the solids are essentially under 50 microns, reblended, and packaged.

EXAMPLE 8 Wettable Powder

    ______________________________________                                         N--[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)-                                                            50%                                                aminocarbonyl]-2-(methylsulfonyl)benzene-                                      sulfonamide                                                                    sodium alkylnaphthalenesulfonate                                                                            2%                                                low viscosity methyl cellulose                                                                              2%                                                diatomaceous earth          46%                                                ______________________________________                                    

The ingredients are blended, coarsely hammer-milled and then air-milled to produce particles essentially all below 10 microns in diameter. The product is reblended before packaging.

EXAMPLE 9 Granule

    ______________________________________                                         Wettable Powder of Example 8                                                                           5%                                                     attapulgite granules   95%                                                     (U.S.S. 20-40 mesh; 0.84-0.42 mm)                                              ______________________________________                                    

A slurry of wettable powder containing ≈25% solids is sprayed on the surface of attapulgite granules in a double-cone blender. The granules are dried and packaged.

EXAMPLE 10 Extruded Pellet

    ______________________________________                                         N--[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)amino-                                                        25%                                               carbonyl]-2-nitrobenzenesulfonamide                                            anhydrous sodium sulfate     10%                                               crude calcium ligninsulfonate                                                                                5%                                               sodium alkylnaphthalenesulfonate                                                                             1%                                               calcium/magnesium bentonite  59%                                               ______________________________________                                    

The ingredients are blended, hammer-milled and then moistened with about 12% water. The mixture is extruded as cylinders about 3 mm diameter which are cut to produce pellets about 3 mm long. These may be used directly after drying, or the dried pellets may be crushed to pass a U.S.S. No. 20 sieve (0.84 mm openings). The granules held on a U.S.S. No. 40 sieve (0.42 mm openings) may be packaged for use and the fines recycled.

EXAMPLE 11 Oil Suspension

    ______________________________________                                         5-chloro-2-[[(4-dimethoxymethyl-6-methoxypyrimidin-2-                                                       25%                                               yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl                            ester                                                                          polyoxyethylene sorbitol hexaoleate                                                                          5%                                               highly aliphatic hydrocarbon oil                                                                            70%                                               ______________________________________                                    

The ingredients are ground together in a sand mill until the solid particles have been reduced to under about 5 microns. The resulting thick suspension may be applied directly, but preferably after being extended with oils or emulsified in water.

EXAMPLE 12 Wettable Powder

    ______________________________________                                         2-[[(4-dimethoxymethyl-6-methoxypyrimidin-2-yl]-                                                         20%                                                  aminocarbonyl]aminosulfonyl]benzoic acid, methyl                               ester                                                                          sodium alkylnaphthalenesulfonate                                                                         4%                                                   sodium ligninsulfonate    4%                                                   low viscosity methyl cellulose                                                                           3%                                                   attapulgite               69%                                                  ______________________________________                                    

The ingredients are thoroughly blended. After grinding in a hammer-mill to produce particles essentially all below 100 microns, the material is reblended and sifted through a U.S.S. No. 50 sieve (0.3 mm opening) and packaged.

EXAMPLE 13 Low Strength Granule

    ______________________________________                                         2-[[[4-methyl-6-(tetrahydropyran-2-yloxymethyl)-                                                          1%                                                  pyrimidin-2-yl]aminocarbonyl]aminosulfonyl]-                                   benzoic acid, methyl ester                                                     N,N--dimethylformamide     9%                                                  attapulgite granules       90%                                                 (U.S.S. 20-40 sieve)                                                           ______________________________________                                    

The active ingredient is dissolved in the solvent and the solution is sprayed upon dedusted granules in a double cone blender. After spraying of the solution has been completed, the blender is allowed to run for a short period and then the granules are packaged.

EXAMPLE 14 Aqueous Suspension

    ______________________________________                                         2-[[[4-(acetyloxymethyl)-6-methylpyrimidin-2-yl]-                                                         40%                                                 aminocarbonyl]aminosulfonyl]benzoic acid,                                      methyl ester                                                                   polyacrylic acid thickener 0.3%                                                dodecylphenol polyethylene glycol ether                                                                   0.5%                                                disodium phosphate          1%                                                 monosodium phosphate       0.5%                                                polyvinyl alcohol          1.0%                                                water                      56.7%                                               ______________________________________                                    

The ingredients are blended and ground together in a sand mill to produce particles essentially all under 5 microns in size.

EXAMPLE 15 Solution

    ______________________________________                                         5-chloro-2-[[(4-dimethoxymethyl-6-methylpyrimidin-2-                                                       5%                                                 yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl                            ester, sodium salt                                                             water                      95%                                                 ______________________________________                                    

The salt is added directly to the water with stirring to produce the solution, which may then be packaged for use.

EXAMPLE 16 Low Strength Granule

    ______________________________________                                         2-[[[4-(dimethoxymethyl)-6-methylpyrimidin-2-yl]-                                                         0.1%                                                aminocarbonyl]aminosulfonyl]benzoic acid,                                      methyl ester                                                                   attapulgite granules      99.9%                                                (U.S.S. 20-40 mesh)                                                            ______________________________________                                    

The active ingredient is dissolved in a solvent and the solution is sprayed upon dedusted granules in a double-cone blender. After spraying of the solution has been completed, the material is warmed to evaporate the solvent. The material is allowed to cool and then packaged.

EXAMPLE 17 Granule

    ______________________________________                                         2-[[(4-(1,3-dioxan-2-yl)-6-methoxypyrimidin-2-yl)-                                                        80%                                                 aminocarbonyl]aminosulfonyl]benzoic acid, methyl                               ester                                                                          wetting agent               1%                                                 crude ligninsulfonate salt (containing                                                                    10%                                                 5-20% of the natural sugars)                                                   attapulgite clay            9%                                                 ______________________________________                                    

The ingredients are blended and milled to pass through a 100 mesh screen. This material is then added to a fluid bed granulator, the air flow is adjusted to gently fluidize the material, and a fine spray of water is sprayed onto the fluidized material. The fluidization and spraying are continued until granules of the desired size range are made. The spraying is stopped, but fluidization is continued, optionally with heat, until the water content is reduced to the desired level, generally less than 1%. The material is then discharged, screened to the desired size range, generally 14-100 mesh (1410-149 microns), and packaged for use.

EXAMPLE 18 High Strength Concentrate

    ______________________________________                                         2-[[(4-(1,3-dioxolan-2-yl)-6-methoxypyrimidin-2-yl)-                                                      99%                                                 aminocarbonyl]aminosulfonyl]benzoic acid, methyl                               ester                                                                          silica aerogel             0.5%                                                synthetic amorphous silica 0.5%                                                ______________________________________                                    

The ingredients are blended and ground in a hammer-mill to produce a material essentially all passing a U.S.S. No. 50 screen (0.3 mm opening). The concentrate may be formulated further if necessary.

EXAMPLE 19 Wettable Powder

    ______________________________________                                         2-[[(4-(1,3-dioxan-2-yl)-6-methoxypyrimidin-2-yl)-                                                        90%                                                 aminocarbonyl]aminosulfonyl]benzoic acid, methyl                               ester                                                                          dioctyl sodium sulfosuccinate                                                                             0.1%                                                synthetic fine silica      9.9%                                                ______________________________________                                    

The ingredients are blended and ground in a hammer-mill to produce particles essentially all below 100 microns. The material is sifted through a U.S.S. No. 50 screen and then packaged.

EXAMPLE 20 Wettable Powder

    ______________________________________                                         2-chloro-N--[[4-(dimethoxymethyl)-6-methylpyrimidin-                                                        40%                                               2-yl]aminocarbonyl]benzenesulfonamide                                          sodium ligninsulfonate       20%                                               montmorillonite clay         40%                                               ______________________________________                                    

The ingredients are thoroughly blended, coarsely hammer-milled and then air-milled to produce particles essentially all below 10 microns in size. The material is reblended and then packaged.

EXAMPLE 21 Oil Suspension

    ______________________________________                                         2-[[[4-(dimethoxymethyl)-6-methylpyrimidin-2-yl]amino-                                                      35%                                               carbonyl]aminosulfonyl]benzoic acid,                                           2-propyl ester                                                                 blend of polyalcohol carboxylic                                                                              6%                                               esters and oil soluble petroleum                                               sulfonates                                                                     xylene                       59%                                               ______________________________________                                    

The ingredients are combined and ground together in a sand mill to produce particles essentially all below 5 microns. The product can be used directly, extended with oils, or emulsified in water.

Utility

The compounds of the present invention are highly active herbicides. They have utility for broad-spectrum pre- and/or post-emergence weed control in areas where complete control of all vegetation is desired, such as around fuel storage tanks, ammunition depots, industrial storage areas, parking lots, drive-in theaters, around billboards, highway and railroad structures. Alternatively, the subject compounds are useful for selective pre- or post-emergence weed control in crops, such as cotton, soybeans and wheat.

The rates of application for the compounds of the invention are influenced by a number of factors, including their use whether as selective or general herbicides, the crop species involved, the types of weeds to be controlled, weather and climate, formulation ingredients, mode of application, amount of foliage present, etc. In general terms, the subject compounds should be applied at levels of around 0.01 to 5 kg/ha, the lower rates being suggested for use on lighter soils and/or those having a low organic matter content, for selective weed control or for situations where only short-term persistence is required.

The compounds of the invention may be used in combination with any other commercial herbicide, such as, for example those listed below.

The compounds of this invention may be used in combination with other commercial herbicides such as:

    ______________________________________                                         Common Name                                                                              Chemical Name                                                        ______________________________________                                         acifluorfen                                                                              5-[2-chloro-4-(trifluoromethyl)phenoxy]-                                       2-nitrobenzoic acid                                                  alachlor  2-chloro-2',6'-diethyl-N--(methoxymethyl)-                                     acetanilide                                                          amitrole  3-amino- .sub.-s-triazole                                            atrazine  2-chloro-4-(ethylamino)-6-(isopropyl-                                          amino)- .sub.-s-triazine                                             barban    4-chloro-2-butynyl  .sub.--m-chlorocarbanilate                       bentazon  3-isopropyl-1H--2,1,3-benzothiadiazin-                                         4(3H)--one 2,2-dioxide                                               benzoylprop                                                                              N--benzoyl-N--(3,4-dichlorophenyl)-DL-                                         alaine                                                               bromacil  5-bromo-3-sec-butyl-6-methyluracil                                   bromoxynil                                                                               3,5-dibromo-4-hydroxybenzonitrile                                    butylate  S--ethyl-diisobutylthiocarbamate                                     CGA 82725 2-(4-(3,5-dichloropyridin-2-yloxy)phen-                                        oxy-propanoic acid, propynyl ester                                   chlortoluron                                                                             N'--(3-chloro-4-methylphenyl-N',N'--                                           dimethylurea                                                         cyanazine 2-[[4-chloro-6-(ethylamino)- .sub.-s-triazin-                                  2-yl]amino]-2-methylpropionitrile                                    diallate  S--(2,3-dichloroallyl)diisopropylthio-                                         carbamate                                                            dicamba   3,6-dichloro- -o-anisic acid                                         dichloroprop                                                                             2-(2,4-dichlorophenoxy)propionic acid                                diclofop  2-[4-(2,4-dichlorophenoxy)phenoxy]-                                            propanoic acid                                                       difenzoquat                                                                              1,2-dimethyl-3,5-diphenyl-1H--pyrazolium                             dinoseb   2-sec-butyl-4,6-dinitrophenol                                        diuron    3-(3,4-dichlorophenyl)-1,1-dimethylurea                              DOWCO 453 2-(4-(3-chloro-5-trifluoromethylpyridin-                             ME        2-yloxy)phenoxy)propanoic acid, methyl                                         ester                                                                EPTC      S--ethyl-dipropylthiocarbamate                                       fenoxaprop                                                                               ethyl 2-(4-(6-chloro-2-benzoxazolyloxy)-                             ethyl     phenoxy)propanoate                                                   flamprop  N--benzoyl-N--(3-chloro-4-fluorophenyl)-DL-                                    alanine                                                              fluazifop-                                                                               butyl 2-[4-[5-(trifluoromethyl)-2-                                   butyl     pyridinyloxy]phenoxy]propanoate                                      fluchloralin                                                                             N--(2-chloroethyl)-2,6-dinitro-N--propyl-4-                                    trifluoromethyl)aniline                                              fluometuron                                                                              1,1-dimethyl-3-(α,α,α-trifluoro-                             .sub.--m-tolyl)-                                                               urea                                                                 FMC 57020 2-(2'chlorophenyl)methyl-4,4-dimethyl-                                         3-isoxazolidinone                                                    fomesafen 5-(2-chloro-4-trifluoromethylphenoxy)-                                         N--methylsulfonyl-2-nitrobenzamide                                   fosamine  ethyl hydrogen (aminocarbonyl)phosphonate                            glyphosate                                                                               N--(phosphonomethyl)glycine                                          hexazinone                                                                               3-cyclohexyl-6-(dimethylamino)-1-methyl-                                       1,3,5-triazine-2,4(1H,3H)--dione                                     ioxynil   4-hydroxy-3,5-diiodobenzonitrile                                     isoproturon                                                                              N--(4-isopropylphenyl)-N',N'--dimethylurea                           lenacil   3-cyclohexyl-6,7-dihydro-1H--cyclopenta-                                       pyrimidine-2,4(3H,5H)--dione                                         MCPA      [(4-chloro- -o-tolyl)oxy]acetic acid                                 MCPB      4-[(4-chloro- -o-tolyl)oxy]propionic acid                            mefluidide                                                                               N--[2,4-dimethyl-5-[[(trifluoromethyl)-                                        sulfonyl]amino]phenyl]acetamide                                      methabenz-                                                                               1,3-dimethyl-3-(2-benzothiazolyl)urea                                thiazuron                                                                      methoxuron                                                                               N'--(3-chloro-4-methoxyphenyl)N,N--                                            dimethylurea                                                         metolachlor                                                                              2-chloro-N--(2-ethyl-6-methylphenyl)-N--(2-                                    methoxy-1-methylethyl)acetamide                                      MSMA      monosodium methanearsonate                                           neburon   1-butyl-3-(3,4-dichlorophenyl)-1-methyl-                                       urea                                                                 oryzalin  3,4-dinitro-N,N--dipropylsulfanilamide                               paraquat  1,1'-dimethyl-4,4'-bipyridinium ion                                  pendimethalin                                                                            N--(1-ethylpropyl)-3,4-dimethyl-2,6-di-                                        nitrobenzeneamine                                                    profluralin                                                                              N--(cyclopropylmethyl)-α,α,α-trifluoro-                      2,6-dinitro-N--propyl- -p-toluidine                                  propanil  3',4'-dichloropropionalide                                           sethoxydim                                                                               2-[1-(ethoxyimino)butyl]-5-[2-(ethyl-                                          thio)propyl]-3-hydroxy-2-cyclohexene-                                          1-one                                                                siduron   1-(2-methylcyclohexyl)-3-phenylurea                                  supriox   2-[1-(2,5-dimethylphenyl)ethylsulfonyl]-                                       pyridine-N--oxide                                                    terbacil  3-tert-butyl-5-chloro-6-methyluracil                                 triallate S--(2,3.3-trichloroallyl)diisopropylthio-                                      carbamate                                                            trifluralin                                                                              α,α,α-trifluoro-2,6-dinitro-N,N--dipropyl-                    -p-toluidine                                                        2,4-D     (2,4-dichlorophenoxy)acetic acid                                     2,4-DB    4-(2,4-dichlorophenoxy)butyric acid                                            3,4-diaryl-4-cyanobutyrates                                                    4-(6-chloroquinoxalinyl-2-oxy)phenoxy-                                         propionate C.sub.1 -C.sub.5 alkyl esters, such                                 as methyl ester, butyl ester, ethyl                                            ester, pentyl ester                                                            ethoxyethoxyethyl 4-(6-chloroquinoxalin-                                       yl-2-oxy)phenoxypropionate                                                     propargyl 2-[4-(3,5-dichloropyridin-2-                                         yloxy)phenoxy]propanoate                                                       methyl 2-[4-(3-chloro-5-trifluoromethyl-                                       pyridin-2-yloxy)phenoxy]propanoate                                   oxyfluorfen                                                                              2-chloro-1-(3-ethoxy-4-nitrophenoxy)-4-                                        (trifluoromethyl)benzene                                             norflurazon                                                                              4-chloro-5-(methylamino)-2-[(3-(tri-                                           fluoro)phenyl]-3(2H)--pyridazinone                                   vernolate S--propyl dipropylthiocarbamate                                                ethyl 5-[2-chloro-4-(trifluoromethyl)-                                         phenoxy]-2-nitrobenzoic acid                                         ______________________________________                                    

The compounds of this invention may particularly be useful in combination with the following herbicides for use as pre-emergent treatments for control of weeds in soybeans:

    ______________________________________                                         Common Name  Tradename  Chemical Name                                          ______________________________________                                         chloramben   Amiben ®                                                                              3-amino-2,5-dichloro-                                                          benzoic acid                                           linuron      Lorox ®                                                                               3-(3,4-dichlorophenyl)-1-                                                      methoxy-1-methylurea                                   metribuzin   Lexone ®                                                                              4-amino-6-tert-butyl-3-                                                        (methylthio)-as-tri-                                                           azin-5(4H)one                                          AC 252,214   --         2-(4,5-dihydro-4-methyl-                                                       4-(1-methylethyl)-5-                                                           oxo-1H--imidazol-2-yl)-                                                        3-quinolinecarboxylic                                                          acid                                                   fomesafen    Flex ® 5-(2-chloro-4-trifluoro-                                                       methylphenoxy)-N--                                                             methylsulfonyl-2-nitro-                                                        benzamide                                              lactofen     --         1'-(carboethoxy)ethyl-5-                                                       (2-chloro-4-(trifluoro-                                                        methyl)phenoxy)-2-                                                             nitrobenzoate                                          ______________________________________                                    

Also preferred are mixtures of some of the compounds of this invention with other sulfonylurea herbicides which may be useful for controlling weeds in soybeans. An example of such a sulfonylurea herbicide is:

2-hydroxy-N-[(4-methoxy-6-methyl-1,3,5-triazin-2-yl)-aminocarbonyl]benzenesulfonamide, 1-propanesulfonate.

The herbicidal properties of the subject compounds were discovered in a number of greenhouse tests. The test procedures and results are shown below.

TEST A

Seeds of crabgrass (Digitaria sp.), barnyardgrass (Echinochloa crusgalli), wild oats (Avena fatua), sicklepod (Cassia obtusifolia), morningglory (Ipomoea sp.), cocklebur (Xanthium sp.), sorghum, corn, soybean, rice, wheat and nutsedge tubers (Cyperus rotundus) were planted in a growth medium and treated pre-emergence with the chemicals dissolved in a non-phytotoxic solvent. At the same time, cotton having five leaves (including cotyledonary ones), bush beans with the third trifoliolate leaf expanding, crabgrass, barnyardgrass and wild oats with two leaves, cassia with three leaves (including cotyledonary ones), morningglory and cocklebur with four leaves (including the cotyledonary ones), sorghum and corn with four leaves, soybean with two cotyledonary leaves, rice with three leaves, wheat with one leaf, and nutsedge with three to five leaves were sprayed. Treated plants and controls were maintained in a greenhouse for sixteen days, whereupon all species were compared to controls and visually rated for response to treatment. The ratings are based on a numerical scale extending from 0=no injury, to 10=complete kill. The accompanying descriptive symbols having the following meanings:

C=chlorosis or necrosis;

D=defoliation;

E=emergence inhibition;

G=growth retardation;

H=formative effects;

S=albinism;

U=unusual pigmentation;

X=axillary stimulation; and

6Y=abscised buds or flowers.

The ratings for the compounds tested by this procedure are presented in Table A.

                                      TABLE A                                      __________________________________________________________________________     Structures                                                                                                           m.p. (°C.)                        __________________________________________________________________________     Compound 1                                                                             ##STR127##                                                             Compound 2                                                                             ##STR128##                                                             Compound 3                                                                             ##STR129##                                                             Compound 4                                                                             ##STR130##                                                             Compound 5                                                                             ##STR131##                                                             Compound 6                                                                             ##STR132##                                                             Compound 7                                                                             ##STR133##                                                             Compound 8                                                                             ##STR134##                                                             Compound 9                                                                             ##STR135##                                                             Compound 10                                                                            ##STR136##                                                             Compound 11                                                                            ##STR137##                                                             Compound 12                                                                            ##STR138##                                                             Compound 13                                                                            ##STR139##                                                             Compound 14                                                                            ##STR140##                                                             Compound 15                                                                            ##STR141##                                                             Compound 16                                                                            ##STR142##                                                             Compound 17                                                                            ##STR143##                                                             Compound 18                                                                            ##STR144##                                                             Compound 19                                                                            ##STR145##                                                             Compound 20                                                                            ##STR146##                                                             Compound 21                                                                            ##STR147##                                                             Compound 22                                                                            ##STR148##                                                             Compound 23                                                                            ##STR149##                                                             Compound 24                                                                            ##STR150##                                                             Compound 25                                                                            ##STR151##                                                             Compound 26                                                                            ##STR152##                                                             Compound 27                                                                            ##STR153##                                                             Compound 28                                                                            ##STR154##                                                             Compound 29                                                                            ##STR155##                                                             Compound 30                                                                            ##STR156##                                                             Compound 31                                                                            ##STR157##                                                             Compound 32                                                                            ##STR158##                                                             Compound 33                                                                            ##STR159##                                                             Compound 34                                                                            ##STR160##                                                             Compound 35                                                                            ##STR161##                                                             Compound 36                                                                            ##STR162##                                                             Compound 37                                                                            ##STR163##                                                             Compound 38                                                                            ##STR164##                                                             Compound 39                                                                            ##STR165##                                                             Compound 40                                                                            ##STR166##                                                             Compound 41                                                                            ##STR167##                                                             Compound 42                                                                            ##STR168##                                                             Compound 43                                                                            ##STR169##                                                             Compound 44                                                                            ##STR170##                                                             Compound 45                                                                            ##STR171##                                                             Compound 46                                                                            ##STR172##                                                             Compound 47                                                                            ##STR173##                                                             Compound 48                                                                            ##STR174##                                                             Compound 49                                                                            ##STR175##                   85                                        Compound 50                                                                            ##STR176##                   182-189(d)                                Compound 51                                                                            ##STR177##                   186-190                                   Compound 52                                                                            ##STR178##                   150- 153                                  Compound 53                                                                            ##STR179##                   130(d)                                    Compound 54                                                                            ##STR180##                   149-152                                   Compound 55                                                                            ##STR181##                   146-149                                   Compound 56                                                                            ##STR182##                   146-149                                   Compound 57                                                                            ##STR183##                   136-146                                   Compound 58                                                                            ##STR184##                   152-156                                   Compound 59                                                                            ##STR185##                   185-188                                   Compound 60                                                                            ##STR186##                    83-85                                    Compound 61                                                                            ##STR187##                    95-100                                   Compound 62                                                                            ##STR188##                   181-183                                   Compound 63                                                                            ##STR189##                   135-138                                   Compound 64                                                                            ##STR190##                   135-138                                   Compound 65                                                                            ##STR191##                   158-163                                   Compound 66                                                                            ##STR192##                   156-158                                   Compound 67                                                                            ##STR193##                   118-119                                   Compound 68                                                                            ##STR194##                   141-143                                   Compound 69                                                                            ##STR195##                   144-146                                   Compound 70                                                                            ##STR196##                    85-90                                    Compound 71                                                                            ##STR197##                    90-95                                    Compound 72                                                                            ##STR198##                   120-128                                   Compound 73                                                                            ##STR199##                   133-138                                   Compound 74                                                                            ##STR200##                   133-138                                   Compound 75                                                                            ##STR201##                   127-133                                   Compound 76                                                                            ##STR202##                   148-154                                   Compound 77                                                                            ##STR203##                   179-185                                   Compound 78                                                                            ##STR204##                                                             Compound 79                                                                            ##STR205##                                                             __________________________________________________________________________

    TABLE A        Cmpd. 1 Cmpd. 2 Cmpd. 3 Cmpd. 4 Cmpd. 5 Cmpd. 6 Cmpd. 7 Cmpd. 8 Cmpd.      9 Cmpd. 10 Cmpd. 11 Cmpd. 12 Cmpd. 13 Cmpd. 14 Cmpd. 15 Cmpd. 16 Rate      kg/ha .05 .05 .05 .05 .05 .05 0.4 0.4 0.4 0.4 0.4 0.4 0.4 .05 .05      0.05     POST-EMERGENCE Bush bean 4C,9G,6Y 5C,9G,6Y 9C 3C,9G,6Y 9C 9C 9C 9      C 9C 9C 9C 9C 9C 9C 9C 4C,9G,6Y Cotton 2C,2H,5G 2C,3H,6G 6C,9G 4C,9H      4C,9G 3C,2H,9G 9C 6C,9G 4C,9H 3C,8G 4C,9G 9C 5C,9G 6C,9G 8C 2C,3H,8G      Morningglory 1C,3G 1C,5G 2C,5G 3C,7H 2C,8G 2C,8H 9C 4C,9G 3C,7G 2C,8G      3C,8H 5C,9G 2C,8H 2C,8G 3C,7G 3C,9G Cocklebur 2C,9G 2C,8G 9C 3C,9H 5C,9G      5C,9G 10C 10C 5C,9G 10C 10C 10C 6C,9G 10C 10C 1C,9G Sicklepod 1C 2C,5G      5C,9G 3C,6G 2C,5G 3C,7G 9C 3C,5G 4C,7G 3C,5H 2C,5G 2C,6G 5C,9G 5C,9G      5C,9G 3C,8G Nutsedge 0 1C,3G 3C,9G 2C,8G 10C 10C 10C 10C 2C,8G 9C 3C,9G      9C 9C 5C,9G 10C 5G Crabgrass 1C,5G 5G 4C,9G 2C,6G 6C,9G 1C,2H 9C 10C      2C,7G 1C,8G 2C,8G 9C 3C,8G 4C,9G 9C 7G Barnyardgrass 2C,9H 2C,9H 9C      5C,9H 9C 3C,9H 9C 10C 9C 9C 6C,9H 9C 10C 9C 9C 2C,9H Wild Oats 1C,3G      2C,8H 9C 3C,8H 2C,9G 3C,9G 9C 5C,9G 2C,9G 3C,9G 3C,9G 9C 9C 9C 4C,9G      2C,9G Wheat 7G,5X 2C,8H 3U,9G 2C,8H 3C,9G 2C,8G 5U,9G 2C,8G 2C,9G 2C,9G      3C,9G 2C,8G 9C 4C,9G 5C,9G 3C,9G Corn 2U,9H 5U,9C 9C 5U,9C 5U,9G 3U,9G      10C 10C 6U,9C 7U,9C 7U,9G 10C 10C 10C 10C 9C Soybean 1G 2C,7G 6C,9G      5C,8H,5X 5C,9G 2C,9G 9C 9C 6U,9G 9C 5C,9G 9C 9C 9C 9C 2C,9G Rice 7G      6C,9G 6C,9G 5C,9G 5C,9G 4C,9G 6C,9G 6C,9G 6C,9G 5C,9G 9C 9C 9C 6C,9G      4C,9G 5C,9G Sorghum 9G 4U,9C 5U,9C 3U,9G 6U,9G 3U,9G 9C 9C 6U,9G 10C 10C      10C 9C 10C 10C 4C,9G Sugar beet                4C,9G PRE-EMERGENCE      Morningglory 6G 3C,5G 8H 3C,5H 8G 1C 2C,9H 4C,9G 8G 8G 7G 9H 8H 8G 8G 9G      Cocklebur 9H 9H 9H 1H 9H 9H -- 9H 9H 5C,9H 9H 9H 9H 9H 9H 7H Sicklepod 0      7G 2C,7G 1C 8G 2C,5G 5C,9G 2C,8G 5G 2C,8G 2C,7G 2C,8G 1C,3G 4C,9G 3C,8G      7H Nutsedge 0 2C,8G 10E 2C,8G 10E 1C,7G 10E 10E 3C,9G 2C,7G 2C,8G 10E      2C,9G 10E 10E 4G Crabgrass 1C,4G 2C 3C,9G 1C 2C,5G 1C 3C,9H 3C,9G 1C,4G      2C,5G 2C,5G 2C,8G 3C,6G 3C,8G 3C,8H 2G Barnyardgrass 4C,7H 3C,9H 6C,9H      3C,9H 5C,8H 2C,6H 5C,9H 3C,9H 5C,9H 5C,9H 3C,9H 2C,9H 5C,9G 5C,9H 5C,9H      8H Wild Oats 2C,7G 2C,9G 5C,9H 2C,9G 2C,9G 2C,8G 4C,9H 3C,9H 2C,9G 2C,9H      9G 3C,9G 3C,9H 4C,9H 5C,9H 8G Wheat 2C,8G 2C,9G 9H 9G 1C,8G 1C,7G 9H 9H      9H 2C,9G 9G 2C,8G 3C,9G 2C,9H 9H 9G Corn 2C,6G 2C,9G 10E 2U,9G 2C,9H      2C,8H 10H 10E 5C,9G 3C,9H 6C,9G 10H 2C,9G 10E 10H 9H Soybean 0 1H 2C,7G      6G 2C,3H 1H 9H 9H 3C,8H 3C,4H 3C,7H 9H 6H 2C,8H 9H 1C,1H Rice 8H 9H 10E      2C,8H 10E 3C,6G 10E 10E 10E 5C,9H 9H 10E 5C,9H 9H 10E 9H Sorghum 2C,8H      5C,9G 10H 2C,9G 2C,9H 2C,9H 7C,9H 3C,9H 10H 10H 4C,9H 5C,9H 2C,9G 3C,9H      5C,9H 9H Sugar beet                8G Cotton         Cmpd. 17 Cmpd. 18 Cmpd. 19 Cmpd. 20 Cmpd. 21 Cmpd. 22 Cmpd. 23 Cmpd.      24 Cmpd. 25 Cmpd. 26 Cmpd. 27 Cmpd. 28 Cmpd. 29 Cmpd. 30 Cmpd. 31 Rate      kg/ha 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05      0.05 0.05        POST-EMERGENCE Bush bean 9C 4S,7G,6Y 4S,2H,6Y 5C,9G,6Y 5C,9G,6Y 9C      4C,9G,6Y 6C,9G,6Y 5C,9G,6Y 5C,9G,6Y 4C,9G,6Y 1C 0 9C 9C Cotton 5C,9G      2C,4G 3C 3C,5G 2C,4G 1C,3G 1C,6G 4C,7G 2C,3G 4C,5G 2C 0 0 5C,9G 3C,5G      Morningglory 5C,9G 3C,6G 3C,8H 3C,9G 3C,8H 2C,8G 5C,8H 4C,9G 4C,8H 5C,8G      2C,2H 0 0 9C 3C,5G Cocklebur 9C 4C,8G 2C,2G 1C,9G 4C,9G 8H 5C,9G 4C,9G      2C,5G 5C,9G 3C,8H 3H 0 10C 9H Sicklepod 6C,9G 2C,3H 2C 3C,5G 5C,9G 3C,9G      4C,9H 3C 2C 3C 2C 0 0 4C,7G 1C,3G Nutsedge 5C,9G 5G 0 2C,9G 2C,9G 9G 9G      0 0 9G 0 0 0 5C,9G 3C,7G Crabgrass 5C,9G 2G 1C 6G 3C,8G 9G 5C,9G 3C,7G 0      2C,8G 0 0 0 3C,9G 2C,5G Barnyardgrass 9C 2C,8H 2C,6H 5C,9H 5C,9H 3C,9H      5C,9H 9C 2C,9H 9C 2C,4H 2H 0 9C 9C Wild Oats 5C,9G 2G 4G 2C,9G 3C,9G      3C,9G 4C,9H 7G 3G 9G 0 0 0 5C,9G 3C,9G Wheat 4C,9G 2G 3G 2C,9G 9G 2C,9G      4C,9G 5G,5X 3G,5X 2C,9G 0 0 0 4C,9G 2C,9G Corn 9C 2C 2C,7H 2C,8H 7U,9C      9C 9C 7U,9C 2C,7H 5U,9C 0 0 0 10C 9C Soybean 5C,9G 2C,4G 1C 2C,9G      2C,8G,5X 9C 3C,8H 5C,9G 1C,1H 4C,8G 4G 0 0 4C,9H 2C,8H Rice 6C,9G 2C,6G      2C,8G 5C,9G 5C,9G 5C,9G 5C,9G 6C,9G 2C,8G 6C,9G 4G 0 0 5C,9G 5C,9G      Sorghum 9C 2C,6H 1C,9G 2C,9H 3C,9G 3C,9G 3C,9G 4C,9G 9G 3U,9G 2C,7H 6G 0      10C 10C Sugar beet 9C 2C,2H 1C,5H 2C,7G 5C,9H 4C,9G 4C,9G 3C,7H 1C,4H 9C      0 -- -- -- -- PRE-EMERGENCE Morningglory 9C 2C,5H 1C,2H 9G 8H,2C 9G 9G      9G 2C,5H 9C 2C,4G 0 0 3C,9H 5G Cocklebur 9H -- 0 9H 9H 9H 9H 9H 7H 8H 8H      8H 0 9H -- Sicklepod 9G 2C 0 5G 1C 6G 5G 8G 2C 8H 1C 2H 5H 3C,8G 2C,7G      Nutsedge 10E 0 0 2C,6G 10E 10E 10E 5G 0 10E 0 0 0 2C,9G 2C Crabgrass 5G      0 0 1C 1C,4G 2C,8G 2C,5G 2G 0 2C,6G 1C 2G 0 3C,8H 2C,5G Barnyardgrass 9H      2C 1C 5C,9H 5C,9H 2C,5G 4C,9H 2C,8G 2C,5G 4C,9H 3C,5G 2G 0 5C,9H 5C,9H      Wild Oats 2C,9G 1C,4G 4G 2C,8G 2C,7G 3C,8G 4C,8H 8G 1C,5G 4C,9H 2C,5G 0      0 5C,9G 5C,9H Wheat 5C,9H 3G 4G 2C,8G 9H 9H 4C,9H 7G 1C,5G 9H 5G 0 0 9H      9H Corn 10H 2C 2C,9H 1C,7G 3C,9G 5C,9H 9H 9G 2C,8H 4C,9H 2C,4G 2G 0 9G      9H Soybean 9H 2G 0 0 0 3C,5H 2C,2H 3C,8H 2G 5G 0 0 0 3C,8H 3C,6G Rice      10E 2G 5G 4C,9H 5G 10E 9H 10E 1C,4G 10E 3C 5G 0 10E 5C,9G Sorghum 10H      1C,9H 2C,9H 2C,8G 3C,9H 7C,9H 5C,9H 3C,9H 4C,9H 10H 2C,5G 2G 0 5C,9H      5C,9H Sugar beet 5C,9G 1C,3H 0 8G 0 10E 10E 5G 0 5C,9G 3C,6G -- -- -- --      Cotton         Cmpd. 32 Cmpd. 33 Cmpd. 34 Cmpd. 35 Cmpd. 36 Cmpd. 37 Cmpd. 38 Cmpd.      39 Cmpd. 40 Cmpd. 41 Cmpd. 42 Cmpd. 43 Cmpd. 44 Cmpd. 45 Cmpd. 46 Rate      kg/ha 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05 0.05      0.05 0.05        POST-EMERGENCE Bush bean 9C 9C 5C,9G,6Y 9C 3C,9G,6Y 4S,8G,6Y 5C,9G,6Y      5C,9G,6Y 5S,8G,6Y 3C,9G,6Y 10D,9G,6Y 9D,9G,6Y 5C,9G,6Y 3C,9G,6Y 9C      Cotton 5C,9G 3C,9G 4C,9G 4C,9G 3C,3H,9G 3C,8G 4C,9G 3C,3H,6G 2C 3C,2H      4C,8G 5C,9G 3C,7G 2C,4G -- Morningglory 5C,9G 2C,8G 3C,5G 9C 3C,7H 3C,7H      5C,9G 3C,8H 2C,5G 2C,5G 9C 3C,8H 1H 1C 10C Cocklebur 10C 9G 3C,9G 2C,9G      2C,2H 2C,3G 5C,9G 3C,6G 2C 3C,5H 9C 6C,9G 5C,9G 4C,9G 10C Sicklepod 9C      4C 2C 2C,7G 2C 2C 4C,8G 2C,5G 3C,5G 2G 3C 3C,6H 5G 3C,4H 9C Nutsedge      2C,9G 5G 2C,9G 9G 0 0 3G 0 4G 3G 1C,9G 9G 0 2C,8G 2C Crabgrass 6C,9G 6G      1C,5G 9G 1C,3G 0 2C,5G 1C 3C,5G 1C,5G 2C,6G 2C,8G 2C,6G 3G 9C Barnyardgra      ss 9C 6C,9H 5C,9H 9C 1C,3G 1C 9C 5C,9H 4C,9H 9H 3C,9H 4C,9H 2C,8H 1H 9C      Wild Oats 9C 2C,9G 1C,8G 3C,9G 5G 2G 1C 0 0 2G 9G 2C,9G 2C,5G 4G 9C      Wheat 9C 9G 4C,9H 3G 0 0 3G 0 0 4G 1C,9G 3C 1C,5G 5G 6C Corn 9C 5C,9G      3C,9H 9C 3C,9H 2C,8H 8U,9C 8U,10C 3U,9C 2C,8H 3C,8H 3C,9H 1U,9G 1C,9G 5C      Soybean 5C,9G 4C,9G 3C,9G,7X 5C,9G 3C,7G,5X 1C,3G 4C,9G 2C,5H 2C,5H 0      5C,9G 9C 4G 2C,9G 10C Rice 9C 5C,9G 6C,9G 5C,9G 2C,7G 2C,9G 3C,8G 2C,6G      2C,8G 2C,9G 5C,9G 6C,9G 3C,9G 2C,8G 6C Sorghum 9C 3C,9G 4C,9G 2C,9G      2C,9G 2C,9H 2C,9G 2C,9G 2C,9G 9G 9G 2C,9G 9G 2C,9H 6C Sugar beet -- --      2C,7G -- -- -- -- -- -- -- -- -- -- -- -- PRE-EMERGENCE Morningglory 9G      8G 1C,4H 9G 0 0 8G 7G 9G 1H 8G 9G 5G 0 10C Cocklebur 9H -- 9H 9H 0 0 7H      0 0 8H 8H 8H 9H 8H 9H Sicklepod 9G 8G 0 7G 1C 0 5G 0 0 0 9C 9G 7G 6G      4C,9G Nutsedge 10E 10E 2C,8G 10E 0 0 0 0 0 0 7G 9G 5G 0 10E Crabgrass      3C,9G 4C,6G 1C,3G 3C,9G 4G,2C 1C 1C,3G 0 1C 1C 5C,8G 4C,8G 2C,8G 1C      5C,9G Barnyardgrass 3C,9H 5C,9H 3C,9H 2C,9H 2C 1C 9G,4C 2C,8G 2C,7G 3C      3C,8G 5C,9H 2C,9H 2C 5C,9H Wild Oats 3C,9H 2C,8G 2C,8H 2C,7G 1C,3G 1C      1C,5G 4G 1C 1C 6G 2C,6G 0 2C 4C,8H Wheat 5C,9H 2C,8H 3C,9H 1C,5G 0 0 4G      2G 3G 6G 8G 2C,9H 8G 5G 3C,9H Corn 9H 2C,9G 3C,9H 2C,9G 2C,9G 2C,9H      2C,9G 4C,9G 2C,9G 2C,4G 2C,7G 8G 3C,7G 2C,8G 3C,9H Soybean 9H 9H 1C,1H      9H 1C 2G 1C,2G 1C 1H 0 6H 6H 0 2H 8H Rice 10E 10E 3C,8H 10E 1C,3G 2G      4C,7H 3C,7H 3C,6G 3C,8H 8H 9H 9H 5G 10E Sorghum 3C,9H 5C,9H 3C,9H 9G      2C,9H 2C 5C,9G 3C,9G 5C,9H 3C,9H 2C,9G 5C,9H 2C,9H 2C,6G 10H Sugar beet      -- -- 8H -- -- -- -- -- -- -- -- -- -- -- -- Cotton        Cmpd. 47 Cmpd. 48 Cmpd. 49 Cmpd. 50 Cmpd. 51 Cmpd. 52 Cmpd. 53 Cmpd.      54 Cmpd. 55 Cmpd. 56 Cmpd. 57 Cmpd. 58 Cmpd. 59 Cmpd. 60 Cmpd. 61 Rate      kg/ha 0.05 0.05 50 50 50 50 50 50 50 50 50 50 50 50 50 400        POST-EMERGENCE Bush bean 5C,9G,6Y 5C,9G,6Y 5C,9G,6Y 4C,9G,6Y 4C,7G,6Y      9C 5C,9G,6Y -- -- -- -- -- -- 6C,9G,6Y -- -- Cotton -- -- 4C,9G 4C,5H,9G      3C,8G 9C 5C,9G 4C,9G 9C 6C,9G 3C,8H 4C,8G 4C,8H 4C,5H 1B 1B Morningglory      10C 5C,9H 5C,9G 4C,9G 3C,8G 5C,9G 5C,9G 6C,9G 4C,8H 5C,9G 3C,6H 3C,6H      4C,7H 3C,4G 1C,3G,1B 1B Cocklebur 10C 5C,9H 4C,9G 9C 7G 2C,9G 9C 5C,9G      10C 10C 4C,9H 3C,9H 4C,8H 5C,9G 1B 1B Sicklepod 4C,8H 3C 3C,9G 3C,7G      1C,3G 3C,3H 2C,5G 3C,7H 5C,9G 9C 5C,9G 3C,3H 9C 2C,4G 1B 1B Nutsedge      3C,8G 3C,9G 2C,9G 6C,9G 3G 3C,8G 2C,9G 3G 2C,9G 3C,8G 0 2G 4C,8G 3C,9G 0      0 Crabgrass 4C,9G 4C,9G 3C,9G 2C,8G 2C,7G 2C,8G 3C,9G 3C,5G 2C,6G 3C,7G      1C,5G 2C,6G 2C,7G 2C,3H 0 1B Barnyardgrass 5C,9G 5C,9H 3C,9H 9C 3C,9H 9C      5C,9H 5C,9H 5C,9G 9C 2C,9H 2C,9H 4C,9H 3C,8H 0 1B Wild Oats 4C,9H 2C,9H      2C,9G 3C,9G 9G 3C,9G 2C,9H 4C,9G 3C,9G 5C,9G 3C,4G 2C 4C,9G 2C,6G 0 1B      Wheat 2C,7G 4C,9G 9C 3C,9G 9G 2C,9G 2C,9G 4C,9G 9C 5C,9G 5G 1C,2G 5C,9G      2C 0 1B Corn 9G 2C,9H 3C,9H 4C,9G 5C,9G 9C 5C,9G 5U,9G 5C,9G 9C 2C,5G      3C,9G 4C,9G 3C,9G 0 1B Soybean 3C,8H 5C,9G 4C,9G 3C,9G 3C,9G 3C,9G 5C,9G      4C,9G 5C,9G 5C,9G 3C,9G 3C,7G 4C,9G 2C,8G 2G,1B 1B Rice 6C,9G 5C,9G      6C,9G 4C,9G 5C,9G 4C,9G 6C,9G 5C,9G 6C,9G 5C,9G 5C,9G 5C,9G 4C,9G 2C,6G      0 1B Sorghum 4C,9G 3C,9G 9C 4C,9G 5C,9G 9C 4C,9G 5C,9G 6C,9G 4C,9G 2C,9H      2C,7H 3C,8G 3C,9G 0 1B Sugar beet -- -- 9C 2C,8G 3C,8H 9C 4C,8H 5C,9G      5C,9G 9C 3C,8G 5C,9G 4C,8G 1H 0 1B PRE-EMERGENCE Morningglory 8H 8H 9G      8G 9C 8G 4C,8H 2C,9G 6G 9G 3C,9H 9G 9G 0 0 0 Cocklebur 9H 9H 9H 2G --      2C,6H -- 9H 9H 9H 9H 9H 9H 2C,6H 0 0 Sicklepod 5H 2C 9G 2C,3G 3C,5G 2C      2C 9G 9G 9G 2C 9G 4C,8H 0 0 0 Nutsedge 10E 10E 10E 9G 2C,5G 2C,6G 5C,9G      4G 9G 8G 5G 2C,7G 0 2C,6G 0 0 Crabgrass 3C,5G 4C,7G 2C,7G 2C,5G 2C,4G      2C,5G 2C,5G 3C,8G 5G 2C,7G 2C,4G 2C,5G 2C,6G 1C 0 0 Barnyardgrass 4C,9H      5C,9H 5C,9H 3C,8H 3C,9G 4C,9G 4C,8G 3C,9H 5C,9H 3C,9H 3C,7H 4C,8G 2C,7G      2C,6H 0 0 Wild Oats 3C,8H 3C,8G 3C,9H 3C,9G 2C,8G 3C,8G 2C,9G 3C,9G      3C,9G 2C,9G 3C,8G 2C,8G 3C,8H 2C,8G 0 0 Wheat 9H 2C,9H 3C,9H 2C,9G 2C,9H      3C,9G 2C,9G 5C,9H 2C,9G 5C,9H 7G 6G 8G 8G 0 0 Corn 4C,9H 3C,9G 3C,9H      2C,9G 5C,9H 3C,9H 3C,9G 4C,9G 2C,9G 3C,9G 2C,7G 2C,9G 3C,8G 5C,9H 0 0      Soybean 1H 2H 3C,8G,7X 2C,2H 3C,6G 2C,8G 3C,5H 3C,4H 2C,7H 3C,6H 2C,2H      2C,8G 3C,5G 0 0 0 Rice 4C,7H 3C,6H 10E 10E 3C,9H 5C,9H 3C,8H 4C,9G 4C,9H      5C,9G 3C,8H 3C,9H 3C,9H 2C,6G 0 0 Sorghum 5C,9H 3C,9H 3C,9H 6C,9H 6C,9H      4C,9H 5C,9G 5C,9G 4C,9H 5C,9G 2C,9H 2C,8H 3C,9H 5C,9H 0 0 Sugar beet --      -- 5C,9G 9C 3C,9G 5C,9G 4C,8G 9C 4C,9G 9C 4C,8G 10E 3C,8G 2G 0 0 Cotton       -- -- -- -- -- 9G 9G 9G 2C,6G 9G 3C,5G -- -- --         Cmpd. Cmpd. Cmpd.                  62 63 64 Cmpd. 65 Cmpd. 66 Cmpd.      67 Cmpd. 68 Cmpd. 69 Cmpd. 70 Cmpd. 71 Cmpd. 72 Cmpd. 73 Cmpd. 74 Cmpd.      75 Cmpd. 76 Cmpd. 77 Cmpd. 78 Cmpd. 79 Rate g/ha 50 50 50 50 50 50 50 50      50 50 50 50 50 50 50 50 50 50        POST-EMERGENCE Bush bean -- -- -- -- -- -- -- -- -- -- -- -- -- -- --      -- -- -- Cotton 2C,9H 9G 5C,9G 3C,8H 3C,8G 2C,9G 3C,9G 5C,9G 5C,9G 9C 2G      3C,9G 2C,5H 3C,8H 1C 2C,5G 4C,9G 4C,8H Morningglory 2H 3C,6G 2C,8G 2C,7H      2C,3G 3C,7H 4G 5C,9G 2C,5G 3C,7H 1H 2C,5G 4G 4C,9G 1C,4G 2C,3H 4C,8H      4C,8H Cocklebur 3C,9H 4C,9H 3C,9H 2C,7H 4C,8G 5C,9G 9C 9C 10C 10C 4C,8H      9C 5G 3C,9H 2C,8H 1H 3C,8H 5C,9G Sicklepod 3C,6H 2C,3G 3C,8H 2C,5G 3C,6H      3C,4G 3C,4G 3C 2C,4G 5C,8G 4C,6H 9C 3G 3C,8G 1C 2C,3H 4C,5H 4C,8H      Nutsedge 0 2C,7G 3C,9G 2G 3G 2C,7G 5C,9G 4C,9G 10C 10C 3G 6C,9G 2G 2C,5G      0 0 2C,4G 0 Crabgrass 0 0 4G 2G 0 3H 4C,6G 6H 8G 2C,8G 1C,3G 2C,7G 2G 2H      0 2G 3C 4C,9G Barnyardgrass 7H 9H 2C,9H 2C,8H 3C,8H 5C,9H 9G 9C 4C,9H      3C,8H 2H 9C 9H 9C 3C,9H 2C,8H 5C,9H 5C,9H Wild Oats 1C 6G 0 0 3G 3C,9G      4C,9G 6C,9G 3C,9G 6C,9G 0 9C 0 5C,9G 1C 2G 4C,9H 4C,8H Wheat 0 0 2C,7G 0      2G 5G 4C,9G 6C,9G 9G 9G 3G 9C 0 5C,9G 1C 3G 9G,7X 8G Corn 2C,7H 3C,9H      3C,9H 3C,8H 3C,8H 5C,9G 10C 10C 5C,9G 5U,9C 0 9C 2C,8H 2C,9H 2C,9H 0      5C,9G 3C,9G Soybean 4C,9G 4C,9G 3C,9G 4C,9G 3C,8G 3C,8H 4C,9G 4C,9G      3C,9G 3C,9G 3C,8H 4C,9G 3C,6H 3C,9G 3C,7H 2H 4C,9G 4C,9G Rice 7G 7G      5C,9G 2C,8G 9G 2C,8G 9C 9C 5C,9G 5C,9G 2C,7G 5C,9G 2C,8G 6C,9G 4C,9G      2C,9G 5C,9G 5C,9G Sorghum 3C,9H 3C,9H 3C,9G 3C,9H 3C,9H 4C,9G 10C 3U,9C      3U,9G 10C 3C,7G 9C 3C,9H 10C 3C,9H 2C,8H 3C,9G 3C,9G Sugar beet 1C,3G      3C,6H 3C,5G 2C,3G 2C,6G 4C,6G 9C 9C 9C 9C 3C,8G 5C,9G 2C,5G 4C,9G 4C,9G      2H 5C,9G 5C,9G PRE-EMERGENCE Morningglory 2C,3H 2C,5H 2C,7G 7H 0 3C,3H      3G 8H 0 9C 1C,2H 8H 2C,5G 9G 9G 0 6H 2C,5H Cocklebur 2C 2C,4H 2C,8H 2H      3C,5H 2C,5H 5C,9H 9H 9H 9C 9H 9H 3C,8H 9H 9H 0 8H 9H Sicklepod 0 0 3C,6G      0 2C 2G 4C,7G 5C,2C 7G 8G 1C 8G 4G 5G 8G 0 3G 2C Nutsedge 0 8G 8G 5G 0 0      10E 10E 10E 10E 0 7G 0 0 0 0 0 0 Crabgrass 0 0 2G 2G 0 0 3G 5G 2C,4G      3C,5G 0 0 2G 0 0 0 1C 0 Barnyardgrass 0 2C,7G 3C,8H 3H 0 3C,8H 9H 3C,9H      3C,8G 3C,8H 2C 3C,9H 1H 2C,3G 2G 0 3C,5H 2C,7G Wild Oats 0 3C,8H 3C,8G      2C,4G 0 3C,8G 3C,9G 3C,9G 3C,8G 4C,9G 3C,7G 4C,9G 0 3C,7G 2C,7G 0 4C,8G      2C,4G Wheat 0 5G 3C,8H 2G 0 8G 2C,9G 2C,9G 6G 3C,9G 3G 2C,9G 0 2C,8G      2C,6G 0 2C,8G 6G Corn 2C,8H 3C,9H 3C,9G 2C,8H 3C,9H 9G 5C,9H 4C,9G 3C,9H      10E 2C,6H 2C,9G 2C,8H 3C,9H 9G 0 3C,9G 3C,8G Soybean 0 0 2C,6H 1C 0      3C,3H 2C,8G 3C,8G 5G 3G 1C,1H 8G 0 3C,7H 5G 0 2C,5G 2C,6G Rice 2G 3C,5G      3C,8H 2C,3G 2C,3G 4C,5G 3C,5G 4C,7G 3C,6H 3C,8H 2C,3H 10E 2C,4G 3C,8H      2C,8G 0 2C,7H 2C,6G Sorghum 2C,7H 9H 4C,9H 3C,8H 3C,8G 4C,9G 6C,9H 6C,9H      6C,9H 5C,9H 3C,8H 3C,9G 2C,9G 2C,9G 2C,5G 0 3C,9G 2C,8H Sugar beet 3H 6G      9G 8G 0 2C,4G 5C,9G 5C,9G 5C,9G 5C,9G 2C,8G 10E 3G 7G 8G 0 3C,9G 3C,8G      Cotton 0 5G 8G 6G 0 6H 8G 9G 9G 9G 0 9G 0 4H 7G 0 2C,3G 5G,2C

TEST B

Two plastic bulb pans were filled with fertilized and limed Fallsington silt loam soil. One pan was planted with corn, sorghum, Kentucky bluegrass and several grass weeds. The other pan was planted with cotton, soybeans, purple nutsedge (Cyperus rotundus), and several broadleaf weeds. The following grass and broadleaf weeds were planted: crabgrass (Digitaria sanguinalis), barnyardgrass (Enchinochloa crussgalli), wild oats (Avena fatua), johnsongrass (Sorghum halepense), dallisgrass (Paspalum dilatatum), giant foxtail (Setaria faberii), cheatgrass (Bromus secalinus), mustard (Brassica arvensis), cocklebur (Xanthium pensylvanicum), pigweed (Amaranthus retroflexus), morningglory, (Ipomoea hederacea), sicklepod (Cassia obtusifolia), teaweed (Sida spinosa), velvetleaf (Abutilon theophrasti), and jimsonweed (Datura stramonium). A 12.5 cm diameter plastic pot was also filled with prepared soil and planted with rice and wheat. Another 12.5 cm pot was planted with sugar beets. The above four containers were treated pre-emergence with several test compounds within the scope of the invention.

Twenty-eight days after treatment, the plants were evaluated and visually rated for response to the chemical treatments utilizing the rating system described previously for Test A. The data are summarized in Table B. At least one compound exhibits utility for pre-emergence weed control in soybeans and cotton.

    TABLE B       PRE-EMERGENCE ON FALLSINGTON SILT LOAM             Cmpd.     Compound 2 Compound 3 Compound 4 Compound 20 Compound      21 22 Compound 23 Compound 24 Compound 26 Compound 30 Rate kg/ha 0.03      0.12 0.03 0.12 0.03 0.12 0.25 0.063 0.125 0.031 0.125 0.125 0.062 0.031      0.015 0.125 0.031 0.062 0.031 0.125 0.031        Crabgrass 0 0 6G,3C 9G,9C 0 0 9G 6G 2G 0 9G 7G 3G 0 0 0 0 8G 5G 7G,2H      7G Barnyardgrass 3G 6G,3H 8G,3H 10C 0 0 9G,9C 8G 3G 0 5G 7G 2G 2G 0 0 0      9G 5G 9G,9C 9G,5H Sorghum 10C 10C 10E 10E 3G 9G,9C 9G,9C 8G 10C 4G 10C      10C 10C 10C 9G 3G 2G 9G,9C 9G 10E 10E Wild Oats 5G 7G 8G,8C 8G,8C 0 6G      8G 6G 8G 4G 8G 9G 7G 5G 4G 0 0 8G 5G 7G 7G Johnsongrass 8G,7C 9G,9C      9G,8C 10C 0 7G,3H 8G 6G 8G 2G 8G 8G 8G 7G 7G 2G 0 9G,9C 7G 9G,9C 8G,7C      Dallisgrass 4G 6G,3H 8G,3H 10C 0 3G 9G 6G 8G 0 9G 9G,9C 8G 5G 3G 0 0 9G      8G 10C 8G,5H Giant foxtail 0 8G,5H 7G,3H 10C 0 3G 9G 2G 0 2G 2G 9G,9C 5G      0 0 0 0 9G,9C 5G 10C 9G,3H Ky. bluegrass 6G 8G,8C 10C 10C 4G 6G,3C 9C,9G      8G 9G 0 9G 9G,9C 8G 3G 3G 0 0 9G,9C 9G 10C 10C Cheatgrass 9G,9C 9G,9C      8G,8C 10C 0 0 9G 7G 8G 4G 9G 9G 8G 6G 4G 0 0 9G,9C 8G 8G,8C 7G Sugar      beets 0 3G 8G,8C 10C 0 0 8G 6G 3G 2G 8G 6G 5G 5G 4G 2G 0 9G 5G 10C 7G,5H      Corn 3G 8G,5H 4G 10C 0 0 8G,7H 5G 6G,5H 0 9G,9C 8G,7H 6G,5H 2G 2G 0 0 9G      9G 10C 3H,8G Mustard 7G,3H 9G,8C 10C 10C 0 6G,3H 9G 9G 9G 7G 9G,9C 9G 9G      7G 5G 0 0 9G,9C 9G 10C 9G,9C Cocklebur 5G 5G 9G,8C 9G,9C 0 0 -- -- 2G 0      5G 6G 3G 3G 2G 0 0 4G 0 8G,8C 7G,5H Pigweed 0 5G,5C 10C 10C 5G,5C 10C --      -- -- -- -- -- -- -- -- -- -- -- -- -- -- Nutsedge 0 3G 7G 10E 0 0 9G 4G      7G 2G 10C 10C 10C 9G 8G 0 0 10C 9G 10E 9G Cotton 0 2G 5G,3H 7G,5H 0 0 5G      2G 2G 0 6G 6G 2G 2G 2G 0 0 4G 0 8G,5H 6G,3H Morningglory 0 4G 2G 3G 0 2G      8G 5G 0 0 6G 4G 3G 2G 0 0 0 7G 4G 9G,7C 6G,5H Sicklepod 0 4G 3G 3G 0 0      5G 2G 5G 2G 2G 0 0 2G 0 0 0 4G 2G 7G,4C 3G Teaweed 0 0 4G,3H 6G,5H 0 0 0      0 0 0 0 2G 0 0 0 0 0 5G 0 7G,3H 4G Velvetleaf 0 0 3G,5H 7G,5H 0 0 7G 2G      0 0 4G 0 0 0 0 0 0 5G 3G 8G,9C 3G Jimsonweed 0 0 3G 7G 0 0 3G 0 0 0 8G 0      0 0 0 0 0 5G 0 9G,8C 3G Soybean 0 0 3G,3H 6G,5H 0 0 3G,3H 0 0 0 7G,7H 2G      2G 0 0 0 0 4G 2G 6G,5H 2C Rice 7G,4C 10C 9G,9C 10C 4G 6G,3H 10C 8G 7G 4G      10C 10C 9G 6G 6G 2G 0 10E 10E 10E 10E Wheat 5G 7G,3C 8G,5C 10C 0 6G,3C      8G 7G 5G 2G 9G 9G 7G 4G 3G 0 0 5G 3G 9G,9C 7G        Compound 31 Compound 32 Compound 33 Compound 35 Compound 38 Compound      39 Compound 42 Rate kg/ha 0.125 0.031 0.125 0.008 0.031 0.003 0.0015      0.125 0.031 0.125 0.008 0.031 0.003 0.0015 0.25 0.062 0.25 0.062 0.125      0.031        Crabgrass 4G 3G 9G,9C 8G 8G 7G 6G 7G 6G 9G 6G 8G 2G 2G 2G 0 2G 0 2G 2G      Barnyardgrass 9G,5H 7G,3H 9G,9C 6G,3C 7G 3G 2G 5H,7G 3H,6G 8G,8C 3G      5H,7G 2G 2G 6G 3G 5G 0 0 0 Sorghum 10E 10C 10C 10C 10C 10C 10C 10C 10C      10C 8G 10C 4G 2G 8G,8C 8G,5H 8G,5H 2G 10C 2G Wild Oats 7G 7G 7G 6G 6G 6G      5G 6G 2G 6G 0 2G 0 0 0 0 0 0 2G 0 Johnsongrass 8G,3H 6G,3H 9G 6G 8G 6G      6G 7G 5G 10C 0 9G 0 0 5G 4G 0 0 2G 0 Dallisgrass 8G,3H 7G,3H 9G,9C 8G      9G,9C 7G 6G 8G 8G 9G,9C 7G 9G 7G 0 0 0 0 0 0 0 Giant foxtail 9G,9C 8G,5H      10C 6G,2H 9G 6G 6G 5G 4G 10C 2G 8G 2G 0 3G 0 0 0 0 0 Ky. bluegrass 10C      7G,3H 10C -- 10C -- -- 9G,9C 9G,9C 9G,9C 4G 9G,9C 2G 0 -- -- -- -- 4G 0      Cheatgrass 8G,9C 6G 10C 9G,5C 10C 9G 5C,8G 10C 10C 9G,9C 9G 10C 8G 4G 3G      0 0 0 2G 0 Sugar beets 7G,5H 4G 10C 10C 9G,9C 9G 8G,8C 9G,9C 7G 10C 9G      10C 8G 7G 4G 2G 4G 0 3G 0 Corn 9G,9C 5H,7G 9G,9C 9G,9C 9G,9C 7H 5G 8G 5G      8G 7G,5H 6G 3G 2G 8G,8C 5G 7G 0 3G 0 Mustard 9G,9C 10C 9G,9C 9G,7C 9G,9C      9G 9G 8G 6G 9C 9G 9G 9G 8G 0 0 0 0 8G 7G Cocklebur 2G 0 8C 6G,2H 7G --      5G,2H 6G 3G 8G,8C 0 6G 3G 0 0 0 0 0 2G 0 Pigweed -- -- -- -- -- -- -- --      -- -- -- -- -- -- -- -- -- -- -- -- Nutsedge 10E 7G 10C 10C 10C 10C 10C      5G 3G 10C 10C 10C 10C 2G 5G 0 0 0 0 0 Cotton 4G 0 8G,8C 8G 7G 8G 6G,3H      6G,3C 3G 8G,8C 6G 7G 3G 0 0 0 2G 0 2G 2G Morningglory 8G,3H 5G 7G 3G,2C      2G 3C 0 6G 0 8G,8C 7G 4G 3G 0 4G 0 2G 0 0 0 Sicklepod 7G 4G 8G,8C 8G,5C      7G,7C 3G 7G 8G,8C 7G,7C 9G,9C 7G 8G,8C 2G 0 0 0 0 0 0 0 Teaweed 8G,3H 3G      8G 8G,3C 8G 8G 7G 8G 7G 10C 3G 9G 0 0 2G 2G -- 2G -- -- Velvetleaf 4G,3H      3G 10C 8G 9G 7G 6G 7G 10C 10C 5G 10C 2G 0 0 0 7G 0 0 2G Jimsonweed 5G,5C      3G 9G,9C 7G,7H 8G,8C 4G 3G 5G 5G 8G 7G 7G 3G 0 0 0 0 0 0 0 Soybean 2G 0      8G,8C 8G,7H 6G,5C 7G 6G,2C 6G,3C 4G 8G,8C 7G,5H 7G,5C 6G 2G 2G 2G 0 0 2G      2G Rice 10C 8G,5H 10C 10C 10C 10C 10C 10C 10C 10C 10C 10C 10C 9G 6G 3G      5G 0 7G 0 Wheat 7G 5G 8G 9G 3G 7G 6G 6G 2G 5G 4G 0 2G 0 0 0 0 0 0      0        Compound 43 Compound 44 Compound 46 Compound 47 Compound 48      Rate kg/ha 0.125 0.031 0.125 0.031 0.125 0.031 0.015 0.125 0.031 0.015      0.125 0.031 0.015        Crabgrass 3G 2G 5G 2G 9G,7C 8G,7C 7G,7C 5G,3C 2C,2G 0 4G 2G 0 Barnyardg      rass 0 0 0 0 9G,7C 8G,7C 5G,3C 6G,3C 2G,2C 0 6G,5C 4G,3C 2G Sorghum      7G,3H 2G 0 0 10C 10C 10C 9G,9C 7G,5H 3G,3H 9G,9C 9G,9C 8G,8C Wild Oats 0      0 0 0 7G,3C 7G,3C 5G,3C 6G 3G 2G 6G 5G 4G Johnsongrass 0 0 0 0 9G,5C      8G,5C 2G 8G,7C 2G 0 8G 8G 3G,3H Dallisgrass 3G 0 2G 0 9G 9G 8G 8G 5G 0      7G 5G 0 Giant foxtail 0 0 0 0 9G,9C 9G,9C 7G 8G,8C 2G,3C 0 8G,8C 4G,3C 0      Ky. bluegrass 2G 0 0 0 -- -- -- -- -- -- -- -- -- Cheatgrass 4G 2G 0 0      8G 8G 2G 8G 5G 0 8G 6G 0 Sugar beets -- -- -- -- 9G,5C 8G,5C 7G 8G 4G,3H      3G 6G 4G 3G Corn 2G 0 0 0 8G,8C 7G,7H 2G,2C 7G,7H 3G,3C 2G,2H 7G,5C      2G,2C 0 Mustard 7G 5G 5G 0 9G,9C 8G,8C 8G,8C 9G,8C 7G 6G 9G,9C 8G,5C 7G      Cocklebur 2G 0 0 0 6G,3C 2G 2G 6G,7C 0 0 5G,5C 3C,2G 0 Pigweed -- -- --      -- -- -- -- -- -- -- -- -- -- Nutsedge 0 0 0 0 10C 9G 6G -- 0 0 -- 2G 2G      Cotton 5G 2G 3G 0 4G,7H 3G,5H 3G 7G,3C 3G 3G 3G,3H 2G 2G Morningglory 2G      0 0 0 7G 5G,5H 3G,3H 5G,3H 0 0 5G 3G 0 Sicklepod 0 0 0 0 -- 5G,5H 3G,3H      2G,3C 0 0 2G 0 0 Teaweed -- -- -- -- -- -- -- -- -- -- -- -- -- Velvetlea      f 0 0 0 0 -- 2G,2H 2G 5G,3H 0 0 7G,5C 0 0 Jimsonweed 0 0 0 0 -- 4G 2G      2G,2C 0 0 2G,2C 0 0 Soybean 0 0 0 0 7H 5G,5H 5G,5H 2G,3C 0 0 2G,3C 0 0      Rice 5G 2G 3G 0 10C 10C 10C 10C 4G 2G 9G 5G 3G Wheat 0 0 0 0 7G 3G 0 7G      4G 2G 5G 4G 4G

TEST C

Two ten-inch in diameter plastic pans lined with polyethylene liners were filled with prepared Fallsington silt loam soil. One pan was planted with seeds of wheat (Triticum aestivum), barley (Hordeum vulgare), wild oats (Avena fatua), downy brome (Bromus tectorum), cheatgrass (Bromus secalinus), blackgrass (Alopecurus myosuroides), annual bluegrass (Poa annua), green foxtail (Setaria viridis), quackgrass (Agropyron repens), Italian ryegrass (Lolium multiflorum) and ripgut brome (Bromus rigidus). The other pan was planted with seeds of Russian thistle (Salsola kali), tansy mustard (Descuraina pinnata), Galium aparine, tumble mustard (Sisymbrium altissium) kochia (Kochia scoparia), shepherd's purse (Capsella bursapastoris), Matricaria inodora, black nightshade (Solanum nigrum), yellow rocket (Barbarea vulgaris), wild mustard (Brassica kaber) and wild buckwheat (Polygonum convolvulus). In certain tests, rapeseed was substituted for wild mustard and Veronica persica was included. The above two pans were treated pre-emergence. At the same time two pans in which the above plant species were growing were treated post-emergence. Plant height at the time of treatment ranged from 1-15 cm depending on plant species.

The test compounds were diluted with a non-phytotoxic solvent and sprayed over-the-top of the pans. An untreated control and a solvent alone control were included for comparison. All treatments were maintained in the greenhouse for 20 days at which time the treatments were compared to the controls and the effects visually rated. The recorded data are presented in Table C. Several of the compounds tested exhibit utility for post-emergence weed control in wheat.

                                      TABLE C                                      __________________________________________________________________________               Compound 1        Compound 35       Compound 35                                Pre-Emergence                                                                          Post-Emergence                                                                          Pre-Emergence     Post-Emergence                    Rate kg/ha                                                                               0.015                                                                              0.06                                                                               0.015                                                                              0.06 0.25                                                                               0.06 0.015                                                                              0.004                                                                               0.25                                                                               0.06 0.015                                                                              0.004                __________________________________________________________________________     wheat     0   0   2G  1C,3G                                                                               7G  5G   1G  0    7G  3G   1G  0                    barley    0   0   4G  6G   8G  --   3G  0    8G  5G   1G  0                    wild oats 0   0   2G  1G   6G  5G   2G  0    7G  5G   2G  0                    downy brome                                                                              0   2G  2G  3G   2C,9G                                                                              2C,8G                                                                               7G  5G   3C,9G                                                                              7G   7G  5G                   cheatgrass                                                                               0   1C,2G                                                                              6G  2C,8G                                                                               10E 10C  1C,8G                                                                              5G   2C,9G                                                                              8G   7G  5G                   blackgrass                                                                               0   0   3G  2C,6G                                                                               4C,9G                                                                              2C,8G                                                                               3C,7G                                                                              5G   9C,9G                                                                              5C,9G                                                                               7C,8G                                                                              1C,5G                annual bluegrass                                                                         0   2G  1C,4G                                                                              8C,9G                                                                               3C,9G                                                                              2C,8G                                                                               8G  4G   2C,8G                                                                              3C,8G                                                                               7G  3G                   green foxtail                                                                            0   0   3G  5G   9G  5C,8G                                                                               2C,7G                                                                              3C,6G                                                                               2C,8G                                                                              2C,8G                                                                               1C,6G                                                                              3G                   quackgrass                                                                               0   0   0   5G   2C,9G                                                                              2C,8G                                                                               8G  5G   1C,6G                                                                              1C,7G                                                                               6G  3G                   Italian ryegrass                                                                         0   1G  3G  9C,9G                                                                               10E 1C,8G                                                                               7G  1C,4G                                                                               2C,7G                                                                              8G   5G  2G                   ripgut brome                                                                             0   0   2G  2C,6G                                                                               3C,9G                                                                              1C,8G                                                                               7G  4G   2C,8G                                                                              7G   5G  5G                   Russian thistle                                                                          0   0   3C,3G                                                                              4G   5C,7G                                                                              2C,6G                                                                               1C,3G                                                                              1C,3G                                                                               9C,9G                                                                              10C  7C,8G                                                                              5C,7G                tansy mustard                                                                            0   --  9G  5G   9C,9G                                                                              7C,9G                                                                               2C,9G                                                                              9G   10C 10C  7C,8G                                                                              5C,7G                Galium aparine                                                                           0   0   2G  2G   3C,9G                                                                              7G   7G  6G   2C,7G                                                                              7G   4G  --                   tumble mustard                                                                           0   0   5G  10C  10C 5C,9G                                                                               9G  8G   10C 10C  10C 5C,8G                kochia    0   0   2G  4G   2C,9G                                                                              9G   8G  6G   10C 9C,9G                                                                               2C,7G                                                                              2C,2G                shepherd's purse                                                                         0   0   10C 2C,2G                                                                               10C 10C  2C,9G                                                                              9G   10C 10C  9C,9G                                                                              7C,9G                Matricaria inodora                                                                       0   0   3G  8C,8G                                                                               9G  9G   8G  7G   7C,9G                                                                              7C,8G                                                                               5C,9G                                                                              3C,8G                black nightshade                                                                         0   0   0   0    3C,9G                                                                              8G   6G  4G   5C,8G                                                                              2C,7G                                                                               2C,7G                                                                              2G                   yellow rocket                                                                            0   0   0   0    3C,9G                                                                              9G   8G  8G   5C,9G                                                                              1C,7G                                                                               2G  0                    wild mustard                                                                             0   0   10C 9G   2C,9G                                                                              9G   1C,9G                                                                              7G   7C,8G                                                                              5C,9G                                                                               2C,7G                                                                              6G                   wild buckwheat                                                                           0   0   1G  0    2C,8G                                                                              8G   5G  2G   10C 6G   3G  --                   Veronica persica                                                               __________________________________________________________________________                                  Compound 43      Compound 46                                                   Pre-Emergence                                                                          Post-Emergence                                                                          Pre-Emergence                                                                          Post-Emergence                              Rate kg/ha                                                                               0.25                                                                               0.06                                                                                0.25                                                                              0.06 0.015                                                                              0.004                                                                              0.015                                                                              0.004                __________________________________________________________________________                        wheat     8G  0   7G  2G   4G  1G  6G  4G                                      barley    2G  2G  3C,5G                                                                              5G   8G  5G  8G  6G                                      wild oats 5G  2G  2C,4G                                                                              2G   8G  5G  3C,8G                                                                              6G                                      downy brome                                                                              8G  4G  4G  4G   9G  7G  3C,8G                                                                              8G                                      cheatgrass                                                                               3C,8G                                                                              2G  4G  2G   2C,8G                                                                              6G  3C,8G                                                                              7G                                      blackgrass                                                                               3C,8G                                                                              2H  8G  2C,5G                                                                               3C,9G                                                                              2C,8G                                                                              10C 3C,8G                                   annual bluegrass                                                                         2C,8G                                                                              4G  4G  2G   4C,9G                                                                              2C,9G                                                                              9C,9G                                                                              3C,8G                                   green foxtail                                                                            2C,5G                                                                              1C,2G                                                                              2C,7G                                                                              2C,4G                                                                               3C,9G                                                                              7G  --  --                                      quackgrass                                                                               5G  2G  --  --   9G  7G  6G  8G                                      Italian ryegrass                                                                         2C,8G                                                                              1C,2G                                                                              1C,2G                                                                              5G   4C,9G                                                                              7G  3C,8G                                                                              7G                                      ripgut brome                                                                             2C,7G                                                                              2G  5G  2G   2C,8G                                                                              6G  2C,8G                                                                              6G                                      Russian thistle                                                                          1C  0   0   0    3G  0   0   0                                       tansy mustard                                                                            9C  9C  2C  1C,2G                                                                               --  --  10C 10C                                     Galium aparine                                                                           7C  3C  3C  3G   5G  5G  6G  3G                                      tumble mustard                                                                           8G  4G  10C 6G   10C 9G  10C 10C                                     kochia    0   0   --  --   8G  0   0   --                                      shepherd's purse                                                                         9G  8G  2C,2G                                                                              5G   10C 9G  10C 8G                                      Matricaria inodora                                                                       9G  6G  5G  1C,3G                                                                               9G  8G  2C,6G                                                                              3G                                      black nightshade                                                                         5G  0   3C,8G                                                                              7G   9G  5G  2C,8G                                                                              6G                                      yellow rocket                                                                            9G  8G  7G  2G   9G  8G  8G  4G                                      rapeseed  9G  7G  8G  3G   9G  8G  6G  5G                                      wild buckwheat                                                                           2G  0   5G  0    7G  5G  10C 2G                                      Veronica persica           --  --  6G  4G                   __________________________________________________________________________

TEST D

The test chemicals, dissolved in a non-phytotoxic solvent, were applied in an overall spray to the foliage and surrounding soil of selected plant species. One day after treatment, plants were observed for rapid burn injury. Approximately fourteen days after treatment, all species were visually compared to untreated controls and rated for response to treatment. The rating system was as described previously for Test A. The data are presented in Table D.

All plant species were seeded in Woodstown sandy loam soil and grown in a greenhouse. The following species were grown in soil contained in plastic pots (25 cm diameter by 13 cm deep): soybeans, cotton, alfalfa, corn, rice, wheat, sorghum, velvetleaf (Abutilon theophrasti), sesbania (Sesbania exaltata), sicklepod (Cassia obtusifolia), morningglory (Ipomoea hederacea), jimsonweed (Datura stramonium), cocklebur (Xanthium pensylvanicum), crabgrass (Digitaria sp.), nutsedge (Cyperus rotundus), barnyardgrass (Echinochloa crusgalli), giant foxtail (Setaria faberii) and wild oats (Avena fatua). The following species were grown in soil in a paper cup (12 cm diameter by 13 cm deep): sunflower, sugar beets, and mustard. All plants were sprayed approximately 14 days after planting. Additional plant species such as johnsongrass, rape and bindweed are sometimes added to this standard test in order to evaluate unusual selectivity.

Several of the compounds tested by this procedure exhibit post-emergence control of weeds in wheat, cotton and soybeans.

                                      TABLE D                                      __________________________________________________________________________             Compound 30                                                                            Compound 31                                                                               Compound 32 Compound 33                                                                            Compound                                                                                Compound 36            Rate kg/ha                                                                             0.015                                                                              0.003                                                                              0.062                                                                              0.015                                                                              0.003                                                                             0.062                                                                              0.015                                                                              0.003                                                                              0.015                                                                              0.003                                                                              0.062                                                                             0.015                                                                              0.003                                                                            0.062                  __________________________________________________________________________     Soybeans                                                                               10G 7G,4C                                                                              7G  2G  0  8G  5G,4C                                                                              4C,4G                                                                              9C  8C  9C 9C 9C 3C,5G                  Velvetleaf                                                                             7G,6C                                                                              0   9G  5G  0  9G  5G,5C                                                                              3G  2C,8G                                                                              2G  9C 8G 6G 1C                     Sesbania                                                                               9G  2G  9G  4G  2G 10C 9C  3C,4G                                                                              10C 8G,6C                                                                              10C                                                                               9G 8G 0                      Sicklepod                                                                              6G,3C                                                                              5G  2G  0   0  2C,5G                                                                              3G,2C                                                                              1C  1G  0   6G 0  0  2C                     Cotton  9G  8G  5G  4G  0  4G,1C                                                                              4C,5G                                                                              3G,3C                                                                              2C  1C  10G                                                                               9G 9G 5G,3C                  Morningglory                                                                           0   6G  3G  2G  0  4G  4G  2G  0   0   9G 9G 8G 6G                     Alfalfa 8G  9G  8G,2C                                                                              3G  8G 4G,3C                                                                              5G,3C                                                                              4G,2C                                                                              3G  2G  9G 9G 7G 3C                     Jimsonweed                                                                             8G  0   3G  2G  0  3G  4G,3C                                                                              2G  2G  1C  9G 9G 7G 7G                     Cocklebur                                                                              8G,3C                                                                              3C  6G  0   0  6G  4G  3G  --  5G  9G 8G 7G 5C,8G                  Corn    9G,8C                                                                              9G,8C                                                                              10G 10C 6G 10C 9C  6G,3C                                                                              1C,3G                                                                              2H,3G                                                                              10C                                                                               9G 8G 8G                     Crabgrass                                                                              7G  0   3G  2G  0  4G  3G  1G  1G  0   9C 8G 4G 0                      Rice    9G,6C                                                                              3C,9G                                                                              8G,6C                                                                              8G,4C                                                                              8G 4G,4C                                                                              7G,5C                                                                              5G,3C                                                                              8C  2G,2C                                                                              9G 8G 8G 6G                     Nutsedge                                                                               0   0   3G  2G  0  5G  3C,3G                                                                              1C,3G                                                                              3C,2G                                                                              0   9C 6C 2G 2G                     Barnyardgrass                                                                          8G,6C                                                                              8G  7G,2C                                                                              6G  2G 10C 6G,3C                                                                              4G  3G  0   10C                                                                               9G 4G 0                      Wheat   5G  3G  6G  4G  2G 5G,4C                                                                              5G  3G  2G  0   6G 0  0  0                      Giant foxtail                                                                          9G,9C                                                                              9G  9G,6C                                                                              7G  4G 10C 8G  3G  7G  2G  10C                                                                               8G 6G 2G                     Wild Oats                                                                              7G  5G  8G  4G  0  6G,3C                                                                              5G  4G  0   0   9G 5G 0  4G                     Sorghum 8G  8G  10C 9G  5G 8C  9C  7G  7G  6G  9G 9G 6G 8G                     Sunflower                                                                              10G 7G,3C                                                                              5G  0   0  10C 3G  3G  0   0   10C                                                                               8G 3G 6C,8G                  Rape    --  --  --  --  -- 8C  4C,7G                                                                              3C,5G                                                                              2G  1G  -- -- -- 5C,6G                  Johnsongrass                                                                           10C 9G  9G,6U                                                                              7G  3G 10C 10C 4C,5G                                                                              4G,4C                                                                              0   9U 7G 0  3G                     Sugar beets                                                                            8G  10C --  --  -- 10C 8C  7G,2C                                                                              2G,3C                                                                              1G,1C                                                                              9G 9G 7G 2C,6G                  Bindweed                                                                               0   0   0   0   0  8G  5G  2C,5G                                                                              0   1C  8G 4G 0  6G                     Mustard 10C 7G,2C                                                                              10C 10C 9G --  --  --  --  --  9G 8G 3G --                     __________________________________________________________________________             Compound 36                                                                           Compound 37                                                                              Compound 39                                                                              Compound 44  Compound 47                    Rate kg/ha                                                                             0.015  0.062                                                                               0.015                                                                               0.062                                                                               0.015                                                                               0.062                                                                               0.015                                                                              0.003                                                                              0.062                                                                               0.015                                                                               0.003                __________________________________________________________________________     Soybeans                                                                               2C,5G  2C,1G                                                                               1G   6G,3C                                                                               6G   0    0   0   10G,7C                                                                              9G,4C                                                                               5G,4C                Velvetleaf                                                                             1G     0    1C   5G,2C                                                                               2G   6G   0   0   8C   6G   4G                   Sesbania                                                                               1G     0    0    9G   7G   6G   0   0   8G   5C   3C                   Sicklepod                                                                              2C     2C,1G                                                                               1G   2G   2G   0    0   0   6C   5C   2C                   Cotton  4G,3C  2G   0    2G   0    9G   9G  2G  9G   9G   6G                   Morningglory                                                                           5G     3C   0    6C,9G                                                                               7G,6C                                                                               3G   0   0   10G  8G   5G                   Alfalfa 2G     2C   0    5G   0    2G   6G  0   8C,8G                                                                               4G   2C                   Jimsonweed                                                                             6G     3G,2C                                                                               1C   3G   3G   0    0   0   7G   6G   2G                   Cocklebur                                                                              5G     3G   0    --   4G   9G   7G  0   10G  7G   3G                   Corn    7G     1C,4G                                                                               1C,3G                                                                               9C,9G                                                                               3C,9G                                                                               8G,2H                                                                               5G  2G  8G,1H                                                                               6G,3H                                                                               0                    Crabgrass                                                                              0      1G   0    6G   2G   8G   5G  2G  6G   3G   0                    Rice    5G     4G   4G   5G,2C                                                                               5G,4C                                                                               5G   2G  2G  9C   9G   4G                   Nutsedge                                                                               0      2G   0    9G,5C                                                                               2G   0    0   0   8G   5G   0                    Barnyardgrass                                                                          0      0    0    9G,8C                                                                               7G   8G   8G  7G  9G   1H,9G                                                                               2G                   Wheat   0      2G   0    0    0    0    0   0   9G   9G   3G                   Giant foxtail                                                                          1G     3G   0    6G   3G   4G   4G  4G  9C,9G                                                                               8G   4G                   Wild Oats                                                                              1G     2G   0    0    0    4G   3G  0   9G   9G   2G                   Sorghum 7G     8G   3G   7G   3G   8G   7G  3G  9G,4U                                                                               9G   9G                   Sunflower                                                                              4G     2C   0    7G,2C                                                                               7G,3C                                                                               8G   8G  0   10C  9G   5G                   Rape    4G,3C  4G,2C                                                                               2G   --   --   --   --  --  --   --   --                   Johnsongrass                                                                           2G     2G,1C                                                                               1G   3G   0    8G   8G  8G  10U  10C  6G                   Sugar beets                                                                            1C,4G  1G   0    4G   4G   8G   8G  7G  9G   7G   0                    Bindweed                                                                               3G     3C,2G                                                                               0    7G   9G   3G   3G  3G  8G   2G   0                    Mustard --     --   --   3G   3G   10C  7G  0   9G   8G   2G                   __________________________________________________________________________

TEST E

For a greenhouse test, a set of 25-cm diameter plastic pots filled with Woodstown sandy loam were planted to Williams soybeans. Similar pots were used to plant the following weed species, three different species per pot: cocklebur (Xanthium pensylvanicum), sicklepod (Cassia obtusifolia), pitted morningglory (Ipomoea lacunosa), johnsongrass (Sorghum halepense), barnyardgrass (Echinochloa crusgalli) and giant foxtail (Setaria faberi). Immediately after planting, the pots were treated pre-emergence with Compound No. 30, dissolved in a non-phytotoxic solvent. The rates of application extended from 4 to 125 g/ha. The treated pots were held in the greenhouse for 27 days and the plants were then rated for response to the chemical treatments. The data are summarized in Table E. Note that Compound No. 30 has potential utility for weed control--particularly grass control-- in soybeans.

                  TABLE E                                                          ______________________________________                                         Pre-emergence on Woodstown Sandy Loam                                          Compound No. 30                                                                          Percent Injury                                                       Rate (g/ha) 4      8      16   31   62   125  --                               ______________________________________                                         Cocklebur   10     40     70   90             0                                Sicklepod    0     20     20   10             0                                Pitted morningglory                                                                         0     20     50   60             0                                Johnsongrass                                                                               90     90     90   95             0                                Barnyardgrass                                                                               0     20     60   95             0                                Giant foxtail                                                                              75     95     95   100            0                                Williams soybeans                   30   60                                    Untreated Control                                                                           0      0      0    0    0    0   0                                ______________________________________                                     

What is claimed is:
 1. A compound of the formula: ##STR206## wherein X is CH₃, OCH₃, Cl, C₂ H₅ or OC₂ H₅ ;Z is CH; Y is CH₂ OR, CH(QR₁)₂, ##STR207## R is C(0)R₃, CO₂ R₄, C(0)NR₅ R₆ or ##STR208## R₁ is C₁ -C₂ alkyl; R₂ is --CH₂ CH₂ --, --CH(CH₃)CH₂ -- or --CH₂ CH₂ CH₂ --; R₃ is C₁ -C₃ alkyl; R₄ is C₁ -C₃ alkyl; R₅ is H or CH₃ ; R₆ is C₁ -C₃ alkyl; Q is O or S; A is ##STR209## R₇ is H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, F, Cl, I, Br, NO₂, CF₃, CO₂ R₉, SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃, OSO₂ R₁₂, S(O)_(n) R₁₃, LCF₃, LCHF₂, LCF₂ CF₂ H, CH₂ Cl, CHCl₂, CH₂ OCH₃ or CH₂ OCH₂ CH₃ ; R₈ is H, F, Cl, Br, CF₃, NO₂, C₁ -C₃ alkyl C₁ -C₃ alkoxy, OCF₂ H or SCF₂ H; R₉ is C₁ -C₄ alkyl, CH₂ CH₂ OCH₃, CH₂ CH₂ Cl or CH₂ CH═CH₂ ; R₁₀ and R₁₁ are independently C₁ -C₃ alkyl; R₁₂ is C₁ -C₄ alkyl, CH₂ CH₂ OCH₃, CH₂ CH₂ CH₂ OCH₃ or C₁ -C₄ alkyl substituted with 1-3 atoms of F, Cl or Br; R₁₃ is C₁ -C₄ alkyl or CH₂ CH═CH₂ ; n is 0 or 2; L is O, S or SO₂ ; R₁₄ is H, CH₃, OCH₃, F, Cl, Br, NO₂, SO₂ N(CH₃)₂, OSO₂ R₁ or S(O)_(n) R₁ ; R₁₅ is H, Cl, Br, CH₃, OCH₃ or NO₂ ; R₁₆ is H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, F, Cl, Br, CF₃, CO₂ R₉, SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃ or S(O)_(n) R₁₃ ; R₁₇ is H, F, Cl, Br, CH₃ or OCH₃ ; W is O or S; W₁ is O or S; R₁₈ is H, C₁ -C₄ alkyl, C₁ -C₄ alkoxy, F, Cl, Br, NO₂, CO₂ R₉, SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃ or S(O)_(n) R₁₃ ; R₁₉ is Cl, NO₂, CF₃, CO₂ R₉, SO₂ N(OCH₃)CH₃, SO₂ NR₁₀ R₁₁, OSO₂ R₁₂, S(O)_(n) R₁₃, C₁ -C₃ alkyl, or C₁ -C₃ alkoxy optionally substituted with 1-5 atoms of Cl or F; R₂₀ is Cl, NO₂, CF₃, CO₂ R₉, SO₂ N(OCH₃)CH₃, C₁ -C₃ alkyl, OSO₂ R₁₂ or C₁ -C₃ alkoxy optionally substituted with 1-5 atoms of Cl or F; R₂₁ is H or CH₃ ;and their agriculturally suitable salts; provided that (1) the total number of carbon atoms of R₁₀ and R₁₁ is less than or equal to 4; (2) when W is O, then R₁₈ is H, Cl, Br, CH₃ or CO₂ R₉ ; (3) when W is O and R₁₈ is H, Cl, Br, or CH₃, then A is ##STR210## and (4) when W₁ is S, then R₂₁ is H and A is ##STR211##
 2. A compound of claim 1 where W₁ is O, X is CH₃, OCH₂ CH₃ or OCH₃ and R₂₁ is H.
 3. A compound of claim 2 where Y is CH(QR₁)₂, CH₂ SR₁, CR₁ (QR₁)₂, ##STR212##
 4. A compound of claim 3 where Y is CH(QR₁)₂, CH₂ SR₁ or ##STR213## and Q is O.
 5. A compound of claim 4 wherein A is ##STR214## R₇ is C₁ -C₃ alkyl, C₁ -C₃ alkoxy, Cl, NO₂, CO₂ R₉, SO₂ (C₁ -C₃ alkyl), SO₂ NR₁₀ R₁₁, SO₂ N(OCH₃)CH₃, OSO₂ R₁₃, CH₂ OCH₃ or LCF₂ H;R₁₄ is CH₃, OCH₃, Cl, OSO₂ CH₃ or SO₂ (C₁ -C₃ alkyl); R₁₆ is CH₃, OCH₃, Cl, SO₂ CH₃ or SO₂ N(CH₃)₂ ; R₁₈ is CH₃, Cl, Br, CO₂ R₉ or SO₂ CH₃.
 6. A compound of claim 5 where A is ##STR215##
 7. A compound of claim 6 whereR₇ is CO₂ CH₃, CO₂ CH₂ CH₃, SO₂ CH₃, SO₂ CH₂ CH₃, SO₂ N(CH₃)₂, OSO₂ CH₃, OSO₂ CH₂ CH₃ ; and R₈ is H, F, Cl, CF₃, CH₃ or OCH₃.
 8. The compound of claim 1 which is 3-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]aminosulfonyl]-2-thiophenecarboxylic acid, methyl ester.
 9. The compound of claim 1 which is 2-chloro-N-[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]benzenesulfonamide.
 10. The compound of claim 1 which is 2-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester.
 11. The compound of claim 1 which is N-[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]-2-methylsulfonylbenzenesulfonamide.
 12. The compound of claim 1 which is N-[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]-2-nitrobenzenesulfonamide.
 13. The compound of claim 1 which is 2-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, 2-propyl ester.
 14. The compound of claim 1 which is 2-[[[4-methyl-6-(tetrahydropyran-2-yloxymethyl)pyrimin-2-yl]aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester.
 15. The compound of claim 1 which is 2-[[[4-(hydroxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester.
 16. The compound of claim 1 which is 2-[[[4-(acetyloxymethyl)-6-methylpyrimidin-2-yl]aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester.
 17. The compound of claim 1 which is 2-[[(4-dimethoxymethyl-6-methoxypyrimidin-2-yl]aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester.
 18. The compound of claim 1 which is 5-chloro-2-[[(4-dimethoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester.
 19. The compound of claim 1 which is 5-chloro-2-[[(4-dimethoxymethyl-6-methoxypyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester.
 20. The compound of claim 1 which is 2-[[(4-(1,3-dioxan-2-yl)-6-methoxypyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester.
 21. The compound of claim 1 which is 2-[[(4-(1,3-dioxolan-2-yl)-6-methoxypyrimidin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid, methyl ester.
 22. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of a compound of claim 1 and at least one of the following: surfactant, solid or liquid inert diluent.
 23. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of a compound of claim 2 and at least one of the following: surfactant, solid or liquid inert diluent.
 24. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of a compound of claim 3 and at least one of the following: surfactant, solid or liquid inert diluent.
 25. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of a compound of claim 4 and at least one of the following: surfactant, solid or liquid inert diluent.
 26. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of a compound of claim 5 and at least one of the following: surfactant, solid or liquid inert diluent.
 27. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 6 and at least one of the following: surfactant, solid or liquid inert diluent.
 28. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 7 and at least one of the following: surfactant, solid or liquid inert diluent.
 29. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 8 and at least one of the following: surfactant, solid or liquid inert diluent.
 30. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 9 and at least one of the following: surfactant, solid or liquid inert diluent.
 31. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 10 and at least one of the following: surfactant, solid or liquid inert diluent.
 32. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 11 and at least one of the following: surfactant, solid or liquid inert diluent.
 33. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 12 and at least one of the following: surfactant, solid or liquid inert diluent.
 34. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 13 and at least one of the following: surfactant, solid or liquid inert diluent.
 35. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 14 and at least one of the following: surfactant, solid or liquid inert diluent.
 36. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 15 and at least one of the following: surfactant, solid or liquid inert diluent.
 37. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 16 and at least one of the following: surfactant, solid or liquid inert diluent.
 38. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 17 and at least one of the following: surfactant, solid or liquid inert diluent.
 39. The composition of claim 38 additionally comprising an effective amount of a compound selected from the group consisting of 3-(3,4-dichlorophenyl)-1-methoxy-1-methylurea, 4-amino-6-tert-butyl-3-(methylthio)-as-triazin-5(4H)-one, and 2-hydroxy-N-[(4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocarbonyl]benzenesulfonamide, 1-propanesulfonate.
 40. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 18 and at least one of the following: surfactant, solid or liquid inert diluent.
 41. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 19 and at least one of the following: surfactant, solid or liquid inert diluent.
 42. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 20 and at least one of the following: surfactant, solid or liquid inert diluent.
 43. A composition suitable for controlling the growth of undesired vegetation which comprises an effective amount of the compound of claim 21 and at least one of the following: surfactant, solid or liquid inert diluent.
 44. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of a compound of claim
 1. 45. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of a compound of claim
 2. 46. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of a compound of claim
 3. 47. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of a compound of claim
 4. 48. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of a compound of claim
 5. 49. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 6. 50. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 7. 51. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 8. 52. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 9. 53. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 10. 54. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 11. 55. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 12. 56. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 13. 57. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 14. 58. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 15. 59. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 16. 60. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 17. 61. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 18. 62. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 19. 63. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 20. 64. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the compound of claim
 21. 65. A method for controlling the growth of undesired vegetation which comprises applying to the locus to be protected an effective amount of the composition of claim
 39. 